Peptide compounds for treatment of no-mediated diseases

ABSTRACT

New peptide compounds of the formula: 
     1. A compound of the formula: ##STR1##

This continuation is a 371 of PCT/JP95/02428 filed Nov. 20, 1995.

TECHNICAL FIELD

This invention relates to new peptide compounds and pharmaceuticallyacceptable salt thereof which are useful as a medicament.

BACKGROUND ART

Some peptide compounds have been known as described, for example, in EP0 394 989 A2.

DISCLOSURE OF INVENTION

This invention relates to new peptide compounds.

One object of this invention is to provide the new and useful peptidecompounds and pharmaceutically acceptable salts thereof which possess astrong inhibitory activity on the production of nitric oxide (NO).

Another object of this invention is to provide process for preparationof the peptide compounds and salts thereof.

A further object o this invention is to provide a pharmaceuticalcomposition comprising said peptide compounds or a pharmaceuticallyacceptable salt thereof.

Still further object of this invention is to provide a use of saidpeptide compounds or a pharmaceutically acceptable salt thereof as amedicament for prophylactic and therapeutic treatment of NO-mediateddiseases such as adult respiratory distress syndrome, cardiovascularischemia, myocarditis, heart failure, synovitis, shock (e.g., septicshock, etc.), diabetes (e.g. insulin-dependent diabetes mellitus, etc.),diabetic nephropathy, diabetic retinopathy, diabetic neuropathy,glomerulonephritis, peptic ulcer, inflammatory bowel disease (e.g.,ulcerative colitis, chronic colitis, etc.), cerebral infarction,cerebral ischemia, migraine, rheumatoid arthritis, gout, neuritis,postherpetic neuralgia, osteoarthritis, osteoporosis, systemic lupuserythematosis, rejection by organ transplantation, asthma, metastasis,Alzheimer's disease, arthritis, CNS disorders, and the like in humanbeing and animals.

The object peptide compounds of the present invention are novel and canbe represented by the following general formula (I) ##STR2## wherein Wis lower alkyl, aryl which may have suitable substituent(s), fluorenylwhich may have suitable substituent(s), heteromonocyclic group which mayhave suitable substituent(s), or a group of the formula: ##STR3## inwhich R¹ is hydrogen, halogen, lower alkyl, nitro, di(lower)alkylamino,amino, protected amino, hydroxyamino or lower alkoxy,

Q is CH or N,

L is a bivalent radical selected from ##STR4## (in which Y is CH or N, Zis NH, O or S, and

--- is a single bond or a double bond) and ##STR5## (in which M is CH orN, and J is CH or N)!,

A¹ is lower alkylene, --NHCO--, ##STR6## (in which V is O or S), or--SO₂ --, T is hydrogen, aryl which may have suitable substituent(s),heterocyclic group, hydroxy, acyloxy, ar(lower)alkoxy, sulfooxy,mercapto, lower alkylthio, mono(or di or tri)ar(lower)alkylthio,acylthio, amino, protected amino, guanidino, acylguanidino or a group ofthe formula: ##STR7## (in which R² is hydroxy, ar(lower)alkoxy,morpholinyl, piperazinyl which may have suitable substituents),piperidyl which may have suitable substituent(s), pyrrolidinyl,thiomorpholinyl, homopiperazinyl which may have suitable substituent(s),piperazinlo which may have suitable substituent(s), piperidyloxy whichmay have suitable substituent(s), or amino having one or two suitablesubstituent(s),

A² is lower alkylene,

R⁸ is hydrogen or lower alkyl, or

R⁸ and a group of the formula: --A² --T are linked together to form##STR8## R³ is hydrogen, aryl which may have suitable substituent(s),hydroxy, protected hydroxy, cyclo(lower)alkyl, lower alkylthio, orheterocyclic group which may have suitable substituent(s),

A³ is bond or lower alkylene,

R⁹ is hydrogen or lower alkyl, or

R⁹ and a group of the formula: --A³ --R³ are linked together to form##STR9## and R⁴ is carboxy, protected carboxy, heterocycliccarbonylwhich may have suitable substituent(s), or a group of the formula:##STR10## (in which R⁵ is hydrogen or lower alkyl, and R⁶ is hydrogen,aryl, ar(lower)alkyl which may have suitable substituent(s),di(lower)alkylamino!(lower)alkyl, or heterocyclic(lower)alkyl which mayhave suitable substituent(s)), or

R⁴ and a group of the formula: --A³ --R³ are linked together to form##STR11## (in which R¹⁰ is ar(lower)alkyl), with proviso that

when M is CH, and J is CH, then Q is N.

The main object compound (I) of the present invention can be prepared bythe following processes.

Process (1) ##STR12## Process (2) ##STR13## Process (3) ##STR14##Process (4) ##STR15## Process (5) ##STR16## wherein W, T, A¹, A², A³, V,R³, R⁴, R⁸ and R⁹ are each as defined above, and

A⁴ is bond or C₁ -C₅ alkylene,

X is a leaving group, ##STR17## is morpholino, piperazino which may havesuitable substituent(s), piperidino which may have suitable substituents), pyrrolidino, thiomorpholino, homopiperazino which may have suitablesubstituent(s), piperazinio which may have suitable substituent(s) oramino having one or two suitable substituent(s).

The other compound (I) of the present invention can be prepared by thefollowing examples or by a conventional method.

The starting compound can be prepared by the following processes.

Process (A) ##STR18## Process (B) ##STR19## Process (C) ##STR20##Process (D) ##STR21## Process (E) ##STR22## wherein R³, R⁴, R⁵, R⁶, R8,R⁹,T, A², A³ ##STR23## and are each as defined above, R⁷ and R¹⁰ areeach amino protective group.

Suitable pharmaceutically acceptable salts of the object compound (I)are conventional non-toxic salts and may include a salt with a base oran acid addition salt such as a salt with an inorganic base, forexample, an alkali metal salt (e.g., sodium salt, potassium salt, etc.),an alkaline earth metal salt (e.g., calcium salt, magnesium salt, etc.),an ammonium salt; a salt with an organic base, for example, an organicamine salt (e.g., triethylamine salt, pyridine salt, picoline salt,ethanolamine salt, triethanolamine salt, dicyclohexylamine salt,N,N'-dibenzylethylenediamine salt, etc.); an inorganic acid additionsalt (e.g., hydrochloride, hydrobromide, sulfate, phosphate, etc.); anorganic carboxylic or sulfonic acid addition salt (e.g., formate,acetate, trifluoroacetate, maleate, tartrate, citrate, fumarate,methanesulfonate, benzenesulfonate, toluenesulfonate, etc.); a salt witha basic or acidic amino acid (e.g., arginine, aspartic acid, glutamicacid, etc.).

In the above and subseauent descriptions of the present specification,suitable examples and illustration of the various definitions which thepresent invention intends to include within the scope thereof areexplained in detail as follows.

The term "lower" is used to intend a group having 1 to 6, preferably 1to 4, carbon atom(s), unless otherwise provided.

The term "higher" is used to intend a group having 7 to 20 carbon atoms,unless otherwise provided.

Suitable "lower alkyl" and "lower alkyl moiety" in the terms"ar(lower)alkyl", "heterocyclic(lower)ialkyl", "di(lower)alkylamino","lower alkylthio", "mono(or di or tri)ar(lower)alkylthio" and "di(lower)alkylamino!(lower)-alkyl" may include straight or branched onehaving 1 to 6 carbon atom(s), such as methyl, ethyl, propyl, isopropyl,butyl, isobutyl, sec-butyl, tert-butyl, pentyl, tert-pentyl, hexyl, andthe like, and in which more preferable example may be C₁ -C₄ alkyl.

Suitable "lower alkenyl" may include vinyl, 1-(or 2-)propenyl, 1-(or 2-or 3-)butenyl, 1-(or 2- or 3- or 4-)pentenyl, 1-(or 2- or 3- or 4- or5-)hexenyl, methylvinyl, ethylvinyl, 1-(or 2- or 3-)methyl-1-(or2-)propenyl, 1-(or 2- or 3-)ethyl-1-(or 2-)propenyl, 1-(or 2- or 3- or4-)methyl-1-(or 2- or 3-)butenyl, and the like, in which more preferableexample may be C₂ -C₄ alkenyl.

Suitable "lower alkynyl" may include ethynyl, 1-propynyl, propargyl,1-methylpropargyl, 1 or 2 or 3-butynyl, 1 or 2 or 3 or 4-pentynyl, 1 or2 or 3 or 4 or 5-hexynyl, and the like.

Suitable "lower alkoxy" and "lower alkoxy moiety" in the term"ar(lower)alkoxy" may include methoxy, ethoxy, propoxy, isopropoxy,butoxy, isobutoxy, t-butoxy, pentyloxy, t-pentyloxy, hexyloxy and thelike.

Suitable "cyclo(lower)alkyl" may include cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cyclohentyl and the like.

Suitable "cyclo(lower)alkenyl" may include cyclohexenyl, cyclohexadienyland the like.

Suitable "aryl" and "aryl moiety" in the terms "ar(lower)alkoxy" and"ark(lower)alkyl" may include phenyl, naphthyl and the like.

Suitable "halogen" may include fluorine, bromine, chlorine and iodine.

Suitable "leaving group" may include acid residue, lower alkoxy asexemplified above, and the like.

Suitable "acid residue" may include halogen as exemplified above,acyloxy and the like.

Suitable "lower alkylene" may include straight or branched one such asmethylene, ethylene, trimethylene, tetramethylene, pentamethylene,hexamethylene, methylmethylene, 1-(or 2-)methyltrimethylene,ethylethylene, propylene, and the like, in which more preferable examplemay be C₁ -C₄ alkylene and the most preferable one may be methylene.

Suitable "C₁ -C₅ alkylene" may include straight or branched one such asmethylene, ethylene, trimethylene, tetramethylene, pentamethylene,methylmethylene, 1-(or 2-)-methyltrimethylene, ethylethylene, propylene,and the like.

Suitable "protected carboxy" may include commonly protected carboxy, andthe like.

Suitable "commonly protected carboxy" may include esterified carboxy andthe like. And suitable example of said ester may be the ones such aslower alkyl ester (e.g., methyl ester, ethyl ester, propyl ester,isopropyl ester, butyl ester, isobutyl ester, t-butyl ester, pentylester, t-pentyl ester, hexyl ester, etc.); lower alkenyl ester (e.g.,vinyl ester, allyl ester, etc.); lower alkynyl ester (e.g., ethynylester, propynyl ester, etc.); lower alkoxy(lower)alkyl ester (e.g.,methoxymethyl ester, ethoxymethyl ester, isopropoxymethyl ester,1-methoxyethyl ester, 1-ethoxyethyl ester, etc.); loweralkylthio(lower)alkyl ester (e.g., methylthiomethyl ester,ethylthiomethyl ester, ethylthioethyl ester, isopropoxythiomethyl ester,etc.); mono(or di or tri)halo(lower)alkyl ester (e.g., 2-iodoethylester, 2,2,2-trichloroethyl ester, etc.); lower alkanoyloxy(lower)alkylester (e.g., acetoxymethyl ester, propionyloxymethyl ester,butyryloxymethyl ester, valeryloxymethyl ester, pivaloyloxymethyl ester,hexanoyloxymethyl ester, 1-acetoxyethyl ester, 2-acetoxyethyl ester,2-propionyloxyethyl ester, etc.); lower alkoxycarbonyloxy(lower)alkylester (e.g., methoxycarbonyloxymethyl ester, ethoxycarbonyloxymethylester, propoxycarbonyloxymethyl ester, 1-(or 2-)-methoxycarbonyloxy!ethyl ester, 1-(or 2-) ethoxycarbonyloxy!ethyl ester,1-(or 2-) propoxycarbonyloxy!ethyl ester, 1-(or 2-)isopropoxycarbonyloxy!ethyl ester, etc.); loweralkanesulfonyl(lower)alkyl ester (e.g., mesylmethyl ester, 2-mesylethylester, etc.); lower alkoxycarbonyloxy(lower)alkyi ester (e.g.,methoxycarbonyloxymethyl ester, ethoxycarbonyloxymethyl ester,propoxycarbonyloxymethyl ester, t-butoxycarbonyloxymethyl ester, 1-(or2-)methoxycarbonyloxyethyl ester, 1-(or 2-)ethoxycarbonyloxyethyl ester,1-(or 2-)isopropoxycarbonyloxyethyl ester, etc.);phthalidylidene(lower)alkyl ester; (5-lower alkyl-2-oxo-1,3-dioxol-4-yl)(lower)alkyl ester e.g., (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester,(5-ethyl-2-oxo-1,3-dioxol-4-yl)methyl ester,(5-propyl-2-oxo-1,3-dioxol-4-yl)ethyl ester, etc.!; mono(or di ortri)aryl(lower)alkyl ester, for example, mono(or di ortri)phenyl(lower)alkyl ester which may have one or more suitablesubstituent(s) (e.g., benzyl ester, 4-methoxybenzyl ester, 4-nitrobenzylester, phenethyl ester, trityl ester, benzhydryl ester,bis(methoxyphenyl)methyl ester, 3,4-dimethoxybenzyl ester,4-hydroxy-3,5-di-t-butylbenzyl ester, etc.); aryl ester which may haveone or more suitable substituent(s) such as substituted or unsubstitutedphenyl ester (e.g., phenyl ester, tolyl ester, t-butylphenyl ester,xylyl ester, mesityl ester, cumenyl ester, 4-chlorophenyl ester,4-methoxyphenyl ester, etc.); tri(lower)alkylsilyl ester; loweralkylthioester (e.g., methylthioester, ethylthioester, etc.) and thelike.

Suitable "hydroxy protective group" in the term "protected hydroxy" mayinclude acyl, mono(or di or tri)phenyl(lower)alkyl which may have one ormore suitable substituent(s) (e.g., benzyl, 4-methoxybenzyl, trityl,etc.), trisubstituted silyl e.g., tri(lower)alkylsilyl (e.g.,trimethylsilyl, t-butyldimethylsilyl, etc.), etc.!, tetrahydropyranyland the like.

Suitable "amino protective group" may include acyl or a conventionalprotective group such as mono(or di or tri)aryl-(lower)alkyl, forexample, mono (or di or tri)phenyl(lower)-alkyl (e.g., benzyl, trityl,etc.) or the like.

Suitable "protected amino" may include acylamino or an amino groupsubstituted by a conventional protecting group such as mono(or di ortri)aryl(lower)alkyl, for example, mono(or di or tri)phenyl(lower)alkyl(e.g., benzyl, trityl, etc.) or the like.

Suitable "acyl" and "acyl moiety" in the terms "acylamino", "acyloxy","acylthio" and "acylguanidino" may include carbamoyl, aliphatic acylgroup and acyl group containing an aromatic ring, which is referred toas aromatic acyl, or heterocyclic ring, whIch is referred to asheterocyclic acyl.

Suitable example of said acyl may be illustrated as follows:

Carbamoyl; Thiocarbamoyl;

Aliphatic acyl such as lower or higher alkanoyl (e.g., formyl, acetyl,propanoyl, butanoyl, 2-methylpropanoyl, pentanoyl,2,2-dimethylpropanoyl, hexanoyl, heptanoyl, octanoyl, nonanoyl,decanoyl, undecanoyl, dodecanoyl, tridecanoyl, tetradecanoyl,pentadecanoyl, hexadecanoyl, heptadecanoyl, octadecanoyl, nonadecanoyl,icosanoyl, etc.); lower or higher alkoxycarbonyl (e.g., methoxycarbonyl,ethoxycarbonyl, t-butoxycarbonyl, t-pentyloxycarbonyl,heptyloxycarbonyl, etc.);

lower or higher alkylsulfonyl (e.g., methylsulfonyl, ethylsulfonyl,etc.);

lower or higher alkoxysulfonyl (e.g., methoxysulfonyl, ethoxysulfonyl,etc.);

cyclo(lower)alkylcarbonyl (e.g., cyclopentylcarbonyl,cyclohexylcarbonyl, etc.); or the like;

Aromatic acyl such as

aroyl (e.g., benzoyl, toluoyl, naphthoyl, etc.);

ar(lower)alkanoyl e.g., phenyl(lower)alkanoyl (e.g., phenylacetyl,phenylpropanoyl, phenylbutanoyl, phenylisobutanoyl, phenylpentanoyl,phenylhexanoyl, etc.), naphthyl(lower)alkanoyl (e.g., naphthylacety,naphthylpropanoyl, naphthylbutanoyl, etc.), etc.!;

ar(lower)alkenoyl e.g., phenyl(lower)alkenoyl (e.g., phenylpropenoyl,phenylbutenoyl, phenylmethacryloyl, phenylpentenoyl, phenylhexenoyl,etc.), naphthyl(lower)alkenoyl (e.g., naphthylpropenoyl,naphthylbutenoyl, etc.), etc.!;

ar(lower)alkoxycarbonyl e.g., phenyl(lower)alkoxycarbonyl (e.g.,benzyloxycarbonyl, etc.), etc.!;

aryloxycarbonyl (e.g., phenoxycarbonyl, naphthyloxycarbonyl, etc.);

aryloxy(lower)alkanoyl (e.g., phenoxyacetyl, phenoxypropionyl, etc.);

arylglyoxyloyl (e.g., phenylglyoxyloyl, naphthylglyoxyloyl, etc.);

arylsulfonyl (e.g., phenylsulfonyl, p-tolylsulfonyl, etc.); or the like;

Heterocyclic acyl such as

heterocycliccarbonyl; heterocyclic(lower)alkanoyl (e.g.,heterocyclicacetyl, heterocyclicpropanoyl, heterocyclicbutanoyl,heterocyclicpentanoyl, heterocyclichexanoyl, etc.);

heterocyclic(lower)alkenoyl (e.g., heterocyclicpropenoyl,heterocyclicbutenoyl, heterocyclicpentenoyl, heterocyclichexenoyl,etc.);

heterocyclicglyoxyloyl; or the like;

in which suitable "heterocyclic moiety" in the terms"heterocycliccarbonyl", "heterocyclic(lower)alkanoyl",heterocyclic(lower)alkenoyl" and "heterocyclicglyoxyloyl" as mentionedabove means, in more detail, saturated or unsaturated, monocyclic orpolycyclic heterocyclic group containing at least one hetero-atom suchas an oxygen, sulfur, nitrogen atom and the like.

And, especially preferable heterocyclic group may be heterocyclic groupsuch as

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 4 nitrogen atom(s), for example,pyrrolyl, pyrrolinyl, imidazolyl, pyrazolyl, pyridyl, dihydropyridyl,pyrimidinyl, pyrazinyl, pyridazinyl, triazolyl (e.g.,4H-1,2,4-triazolyl, 1H-1,2,4-triazolyl, 1H-1,2,3-triazolyl,2H-1,2,3-triazolyl, etc.), tetrazolyl (e.g., 1H-tetrazolyl,2H-tetrazolyl, etc.), etc.;

saturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 4 nitrogen atom(s), for example,pyrrolidinyl, imidazolidinyl, piperidyl, piperazinyl, etc.;

unsaturated condensed heterocyclic group containing 1 to 4 nitrogenatom(s), for example, indolyl, isoindolyl, indolinyl, indolizinyl,benzimidazolyl (e.g. 1H-benzimidazolyl, etc.), quinolyl, isoquinolyl,tetrahydroisoquinolyl (e.g. 1,2,3,4-tetrahydroisoquinolyl, etc.)indazolyl, benzotriazolyl, quinazolinyl, quinoxalinyl, phthalazinyl,etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3nitrogen atom(s), for example, oxazolyl, isoxazolyl, oxadiazolyl (e.g.,1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, etc.), etc.;

saturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3nitrogen atom(s), for example, morpholinyl, sydnonyl, etc.;

unsaturated condensed heterocyclic group containing 1 to 2 oxygenatom(s) and 1 to 3 nitrogen atom(s), for example, benzoxazolyl,benzoxadiazolyl, etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3nitrogen atom(s), for example, thiazolyl, isothiazolyl, thiadiazolyl(e.g., 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl,1,2,5-thiadiazolyl, etc.), dihydrothiazinyl, etc.;

saturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3nitrogen atom(s), for example, thiomorpholinyl, thiazolidinyl, etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 sulfur atom(s), for example,thienyl, dihydrodithiinyl, dihydrodithionyl, etc.;

unsaturated condensed heterocyclic group containing 1 to 2 sulfuratom(s) and 1 to 3 nitrogen atom(s), for example, benzothiazolyl,benzothiadiazolyl, etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing an oxygen atom, for example, furyl,etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing an oxygen atom and 1 to 2 sulfuratom(s), for example, dihydrooxathiinyl, etc.;

unsaturated condensed heterocyclic group containing 1 to 2 sulfuratom(s), for example, benzothienyl, benzodithiinyl, etc.;

unsaturated condensed heterocyclic group containing an oxygen atom and 1to 2 sulfur atom(s), for example, benzoxathiinyl, etc.; and the like.

The acyl moiety as stated above may have one to ten, same or different,suitable substituent(s) such as lower alkyl as exemplified above, loweralkoxy as exemplified above, lower alkylthio wherein lower alkyl moietyis as exemplified above, lower alkylamino wherein lower alkyl moiety isas exemplified above, di(lower)alkylamino wherein lower alkyl moiety isas exemplified above, cyclo(lower)alkyl as exemplified above,cyclo(lower)alkenyl as exemplified above, halogen as exemplified above,aryl as exemplified above, amino, protected amino as exemplified above,hydroxy, protected hydroxy as exemplified above, cyano, nitro, carboxy,protected carboxy as exemplified above, sulfo, sulfamoyl, imino, oxo,aminc(lower)alkyl wherein lower alkyl moiety is as exemplified above,carbamoyloxy, mono(or di or tri)halo(lower)alkyl wherein halogen moietyand lower alkyl moiety are each as exemplified above,hydroxy(lower)alkyl wherein lower alkyl moiety is as exemplified above,or the like.

Suitable "heterocyclic group" and "heterocyclic moiety" in the terms"heterocycliccarbonyl" and "heterocyclic(lower)alkyl" can be referred tothe ones as exemplified above.

Suitable "commonly protected amino" may include amino substituted with acommon N-protective group such as substituted or unsubstituted loweralkanoyl (e.g., formyl, acetyl, propionyl, trifluoroacetyl, etc.),phthaloyl, lower alkoxycarbonyl (e.g., tert-butoxycarbonyl,tert-amyloxycarbonyl, etc.), substituted or unsubstitutedar(lower)alkanoyl (e.g., benzyloxycarbonyl, p-nitrobenzyloxycarbonyl,etc.), carbamoyl, substituted carbamoyl e.g., mono or di(loweralkyl)carbamoyl (e.g., methylcarbamoyl, dimethylcarbamoyl, etc.),arylcarbamoyl (e.g., phenylcarbamoyl, etc.), etc.!, substituted orunsubstituted arylsulfonyl (e.g., phenylsulfonyl, tosyl, etc.),nitrophenylsulfenyl, ar(lower)alkyl (e.g., trityl or benzyl, etc.), orthe like.

Suitable "heteromonocyclic group" may include

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 4 nitrogen atom(s), for example,pyrrolyl, pyrrolinyl, imidazolyl, pyrazolyl, pyridyl, dihydropyridyl,pyrimidinyl, pyrazinyl, pyridazinyl, triazolyl (e.g.,4H-1,2,4-triazolyl, 1H-1,2,3-triazolyl, 2H-1,2,3-triazolyl, etc.),tetrazolyl (e.g., 1H, tetrazolyl, 2H-tetrazolyl, etc.), etc.;

saturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 4 nitrogen atom(s), for examplepyrrolidinyl, imidazolidinyl, piperidyl, piperazinyl, etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3nitrogen atom(s), for example, oxazolyl, isoxazolyl, oxadiazolyl (e.g.,1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyi, etc.), etc.;

saturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3nitrogen atom(s), for example, morpholinyl, sydnonyl, etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3nitrogen atom(s), for example, thiazolyl, isothiazolyl, thiadiazolyl(e.g., 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl,1,2,5-thiadiazolyl, etc.), dihydrothiazinyl, etc.;

saturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3nitrogen atom(s), for example, thiazolidinyl, etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heterorionocyclic group containing 1 to 2 sulfur atom(s), for example,thienyl, dihydrodithiinyl, dihydrodithionyl, etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing an oxygen atom, for example, furyl,etc.;

unsaturated 3 to 8-membered (more preferably 5 or 6-membered)heteromonocyclic group containing an oxygen atom and 1 to 2 sulfuratom(s), for example, dihydrooxathiinyl, etc.; and the like.

Suitable "substituent" in the terms "aryl which may have suitablesubstituent(s)", "fluorenyl which may have suitable substituent(s)","piperidyl which may have suitable substituent(s)", "piperazanyl whichmay have suitable substituent(s)", "piperazinio which may have suitablesubstituent(s)", "homopiperazinyl which may have suitablesubstituent(s)", "piperidyloxy which may have suitable substituentfs)","amino having one or two suitable substituent(s)", "heterocyclic groupwhich may have suitable substituent(s)", "ar(lower)alkyl which may havesuitable substituent(s)", "heterocycliccarbonyl which may have suitablesubstituent(s)", "heterocyclic(lower)alkyl which may have suitablesubstituent(s)", "heteromonocyclic group which may have suitablesubstituent(s)", "piperaziro which may have suitable substituent(s)","piperidino which may have suitable substituent(s)" and "homopiperidinowhich may have suitable substituent(s)" may include lower alkyl asexemplified above, lower alkoxy as exemplified above, lower alkenyl asexemplified above, lower alkynyl as exemplified above, mono(or di ortri)halo(lower)alkyl wherein halogen moiety and lower alkyl moiety areeach as exemplified above, cyclo (lower) alkyl as exemplilied above,cyclo (lower) alkenyl as exemplified above, halogen as exemplifiedabove, carboxy, protected carboxy as exemplified above, hydroxy,protected hydroxy as exemplified above, aryl as exemplified above,ar(lower)alkyl wherein aryl moiety and lower alkyl moiety are each asexemplified above, carboxy(lower)alkyl wherein lower alkyl moiety asexemplified above, protected carboxy(lower)alkyl wherein protectedcarboxy moiety and lower alkyl moiety are each as exemplified above,nitro, amino, protected amino as exemplified above, di(lower)alkylaminowherein lower alkyl moiety is as exemplified above, amino(lower)alkylwherein lower alkyl moiety is as exemplified above, protectedamino(lower)alkyl wherein protected amino moiety and lower alkyl moietyare each as exemplified above, acyl as exemplified above, cyano, sulfo,oxo, sulfamoyl, carbamoyloxy, mercapto, lower alkylthio wherein loweralkyl moiety is as exemplified above, hydroxy, protected hydroxy asexemplified above, heterocyclic group which may have lower alkyl whereinheterocyclic moiety and lower alkyl moiety are each as exemplifiedabove, imino, di(lower)alkylamino!(lower)alkyl wherein lower alkylmoiety is as exemplified above, di(lower)alkylamino!(lower)alkoxywherein lower alkyl moiety and lower alkoxy moiety are each asexemplified above, mono(or di or tri)(protected hydroxy)(lower)alkylwherein protected hydroxy moiety and lower alkyl moiety are each asexemplified above, mono(or di or tri)(hydroxy)(lower)alkyl wherein loweralkyl moiety is as exemplified above, methylenedioxy and the like.

The processes for preparing the object and starting compounds areexplained in detail in the following.

Process (1)

The compound (Ic) or a salt thereof can be prepared by reacting thecompound (II) or its reactive derivative or a salt thereof with thecompound (III) or its reactive derivative at the carboxy group, or asalt thereof.

Suitable reactive derivative of the compound (II) may include Schiff'sbase type imino or its tautomeric enamine type isomer formed by thereaction of the compound (II) with a carbonyl compound such as aldehyde,ketone or the like; a silyl derivative formed by the reaction of thecompound (II) with a silyl compound such as N,O-bis(trimethylsilyl)acetamide, N-trimethylsilylacetamide or the like; aderivative formed by the reaction of the compound (II) with phosphorustrichloride or phosgene, and the like.

Suitable reactive derivative of the compound (III) may include an acidhalide, an acid anhydride, an activated ester, and the like. Thesuitable example may be an acid chloride; acid azide; a mixed acidanhydride with an acid such as substituted phosphoric acid (e.g.,dialkylphosphoric acid, phenylphosphoric acid, diphenylphosphoric acid,dibenzylphosphoric acid, halogenated phosphoric acid, etc.),dialkylphosphorous acid, sulfurous acid, thiosulfuric acid,alkanesulfonlc acid (e.g., methanesulfonic acid, ethanesulfonic acid,etc.), sulfuric acid, alkylcarbonic acid, aliphatic carboxylic acid(e.g., pivalic acid, pentanoic acid, isopentanoic acid, 2-ethylbutyricacid, trichloroacetic acid, etc.); aromatic carboxylic acid (e.g.,benzoic acid, etc.); a symmetrical acid anhydride; an activated amidewith imidazole, 4-substituted imidazole, dimethylpyrazole, triazole ortetrazole; an activated ester (e.g., cyanomethyl ester, methoxymethylester, dimethyliminomethyl (CH₃)₂ ⁺ N═CH--! ester, vinyl ester,propargyl ester, p-nitrophenyl ester, 2,4-dinitrophenyl ester,trichlorophenyl ester, pentachlorophenyl ester, mesylphenyl ester,phenylazophenyl ester, phenylthio ester, p-nitrophenyl thioester,p-cresyl thioester, carboxymethyl thioester, pyranyl ester, pyridylester, piperidyl ester, 8-quinolyl thioester, etc.); an ester with aN-hydroxy compound (e.g., N,N-dimethylhydroxylamlne,1-hydroxy-2-(1H)-pyridone, N-hydroxysuccinimide, N-hydroxybenzotriazole,N-hydroxyphthalimide, 1-hydroxy-6-chloro-1H-benzotriazole, etc.); andthe like. These reactive derivatives can optionally be selected fromthem according to the kind of the compound (III) to be used.

The reaction is usually carried out in a conventional solvent such aswater, acetone, dioxane, acetonitrile, chloroform, methylene chloride,ethylene chloride, tetrahydrofuran, ethyl acetate,N,N-dimethylformamide, pyridine or any other organic solvents which donot adversely affect the reaction, or the mixture thereof.

When the compound (III) is used in free acid form or its salt form inthe reaction, the reaction is preferable carried out in the presence ofa conventional condensing agent such as N,N'-dicyclohexylcarbodiimide;N-cyclohexyl-N'-morpholinoethylcarbodiimide;N-cyclohexyl-N'-(4-diethylaminocyclohexyl) carbodiimide;N,N'-diisopropylcarbodiimide;N-ethyl-N'-(3-dimethylaminopropyl)carbodiimide;N,N-carbonyl-bis(2-methylimidazole);pentamethyleneketene-N-cyclohexylimine;diphenylketene-N-cyclohexylimine; ethoxyacetylene;1-alkoxy-1-chloroethylene; trialkyl phosphite; isopropyl polyphosphate;phosphorous oxychloride (phosphoryl chloride); phosphorous trichloride;thionyl chloride; oxalyl chloride; triphenylphosphite;2-ethyl-7-hydroxybenzisoxazolium salt;2-ethyl-5-(m-sulfophenyl)isoxazolium hydroxide intra-molecular salt;1-(p-chlorobenzenesulfonyloxy)-6-chloro-1H-benzotriazole; so-calledVilsmeier reagent prepared by the reaction of N,N-dimethylformamide withthionyl chloride, phosgene, phosphorous oxychloride, etc.; or the like.

The reaction may be also be carried out in the presence of an organic orinorganic base such as an alkali metal bicarbonate, tri(lower)alkylamine, pyridine, N-(lower)-alkylmorphorine,N,N-di(lower)alkylbenzylamine, or the like.

The reaction temperature is not critical, and the reaction is usuallycarried out under cooling to heating.

Process (2)

The compound (Ib) or a salt thereof can be prepared by reacting thecompound (Ia) or its reactive derivative at the carboxy group, or a saltthereof with the compound (IV) or its reactive derivative, or a saltthereof.

This reaction can be carried out in a similar manner to that of theaforementioned Process (1), and therefore the reagents to be used andthe reaction conditions (e.g., solvent, reaction temperature, etc.) canbe referred to those of the Process (I).

Process (3)

The compound (Id) or a salt thereof can be prepared by reacting thecompound (II) or a salt thereof with the compound (XI) or a saltthereof.

The reaction can be carried out in the manner disclosed in Example 12 orsimilar manners thereto.

Process (4)

The compound (Ie) or a salt thereof can be prepared by reacting thecompound (II) or a salt thereof with the compound (XII) and then bysubjecting the resultant compound to reduction reaction.

The reaction can be carried out in the manner disclosed in Example 13 orsimilar manners thereto.

Process (5)

The compound (If) or a salt thereof can be prepared by reacting thecompound (II) or a salt thereof with the compound (XIII) or a saltthereof.

The reaction can be carried out in the manner disclosed in Example 39 orsimilar manners thereto.

Process (A)

The compound (IIb) or a salt thereof can be prepared by reacting thecompound (IIa) or its reactive derivative at the carboxy group, or asalt thereof with the compound (IV) or its reactive derivative, or asalt thereof.

This reaction can be carried out in a similar manner to that of theaforementioned Process (1), and therefore the reagents to be used andthe reaction conditions (e.g., solvent, reaction temperature, etc.) canbe referred to those of the Process (1).

Process (B)

The compound (II) or a salt thereof can be prepared by subjecting thecompound (V) or a salt thereof to elimination reaction of the aminoprotective group.

Suitable method of this elimination reaction may include conventionalone such as hydrolysis, reduction and the like.

(i) For Hydrolysis:

The hydrolysis is preferably carried out in the presence of a base or anacid including Lewis acid.

Suitable base may include an inorganic base and an organic base such asan alkali metal e.g., sodium, potassium, etc.!, an alkaline earth metale.g., magnesium, calcium, etc.!, the hydroxide or carbonate orhydrogencarbonate thereof, trialkylamine e.g., trimethylamine,triethylamine, etc.!, picoline, 1,5-diazabicyclo 4.3.0!-non-5-ene, orthe like.

Suitable acid may include an organic acid e.g., formic acid, aceticacid, propionic acid, trichloroacetic acid, trifluoroacetic acid, etc.!,and an inorganic acid e.g., hydrochloric acid, hydrobromic acid,sulfuric acid, hydrogen chloride, hydrogen bromide, etc.!.

The elimination using Lewis acid such as trihaloacetic acid e.g.,trichloroacetic acid, trifluoroacetic acid, etc.!, or the like ispreferably carried out in the presence of cation trapping agents e.g.,anisole, phenol, etc.!. This reaction is usually carried out in nosolvent.

The reaction may be carried out in a conventional solvent such as water,alcohol (e.g., methanol, ethanol, isopropyl alcohol, etc.),tetrahydrofuran, dioxane, toluene, methylene chloride, ethylenedichloride, chloroform, N,N-dimethylformamide, N,N-dimethylacetamide orany other organic solvents which do not adversely affect the reaction,or the mixture thereof.

The reaction temperature is not critical and the reaction is usuallycarried out under cooling to warming.

(ii) For reduction:

Reduction is carried out in a conventional manner, including chemicalreduction and catalytic reduction.

Suitable reducing reagent to be used in chemical reduction are hydrides(e.g., hydrogen iodide, hydrogen sulfide, lithium aluminum hydride,sodium borohydride, sodium cyanoborohydride, etc.), or a combination ofa metal (e.g., tin, zinc, iron, etc.) or metallic compound (e.g.,chromium chloride, chromium acetate, etc.) and an organic acid or aninorganic acid (e.g., formic acid, acetic acid, propionic acid,trifluoroacetic acid, p-toluenesulfonic acid, hydrochloric acid,hydrobromic acid, etc.).

Suitable catalysts to be used in catalytic reduction are conventionalones such as platinum catalysts (e.g., platinum plate, spongy platinum,platinum black, colloidal platinum, platinum oxide, platinum wire,etc.), palladium catalysts (e.g., spongy palladium, palladium black,palladium oxide, palladium on carbon, colloidal palladium, palladium onbarium sulfate, palladium on barium carbonate, etc.), nickel catalysts(e.g., reduced nickel, nickel oxide, Raney nickel, etc.), cobaltcatalysts (e.g., reduced cobalt, Raney cobalt, etc.), iron catalysts(e.g., reduced iron, Raney iron, Ullman iron, etc.), and the like.

The reduction is usuallv carried out in a conventional solvent such aswater, alcohol (e.g., methanol, ethanol, isopropyl alcohol, etc.),tetrahydrofuran, dioxane, toluene, methylene chloride, ethylenedichloride, chloroform, N,N-dimethylformamide, N,N-dimethylacetamide orany other organic solvents which do not adversely affect the reaction,or the mixture thereof.

Additionally, in case that the above-mentioned acids to be used inchemical reduction are in liquid, they can also be used as a solvent.

The reaction temperature of this reduction is not critical and thereaction is usually carried out under cooling to warming.

Process C

The compound (VIIIa) or a salt thereof can be prepared by reacting thecompound (VI) or its reactive derivative at the carboxy group, or a saltthereof with the compound (VII) or its reactive derivative, or a saltthereof.

This reaction can be carried out in a similar manner to that of theaforementioned Process (1), and therefore the reagents to be used andthe reaction conditions (e.g., solvent, reaction temperature, etc.) canbe referred to those of the Process (1).

Process (D)

The compound (IX) or a salt thereof can be prepared by subjecting thecompound (VIII) or a salt thereof to elimination reaction of the aminoprotective group.

This reaction can be carried out in a similar manner to that of theaforementioned Process (B), and therefore the reagents to be used andthe reaction conditions (e.g., solvent, reaction temperature, etc.) canbe referred to those of the Process (B).

Process (E)

The compound (V) or a salt thereof can be prepared by reacting thecompound (IX) or its reactive derivative, or a salt thereof with thecompound (X) or its reactive derivative at the carboxy group, or a saltthereof.

This reaction can be carried out in a similar manner to that of theaforementioned Process (1), and therefore the reagents to be used andthe reaction conditions (e.g., solvent, reaction temperature, etc.) canbe referred to those of the Process (1).

Suitable salts of the object, starting compounds and their reactivederivatives in Processes (1)˜(5) and (A)˜(E) can be referred to the onesas exemplified for the compound (I).

The compounds obtained by the above processes can be isolated andpurified by a conventional method such as pulverization,recrystallization, column chromatography, reprecipitation, or the like.

It is to be noted that the compound (I) and the other compounds mayinclude one or more stereoisomer(s) such as optical isomer(s) andgeometrical isomer(s) due to asymmetric carbon atom(s) and doublebond(s), and all of such isomers and mixture thereof are included withinthe scope of this invention.

The object compounds (I) and pharmaceutically acceptable salts thereofpossess a strong inhibitory activity on the production of nitric oxide(NO).

Accordingly, the object compounds (I) and pharmaceutically acceptablesalts thereof are expected to possess a nitric oxide synthase(NOS)-inhibitory activity or a NOS-production inhibitory activity.

Accordingly, they are useful for prevention and/or treatment ofNO-mediated diseases such as adult respiratory distress syndrome,cardiovascular ischemia, myocarditis, heart failure, synovitis, shock(e.g., septic shock, etc.), diabetes (e.g., insulin-dependent diabetesmellitus, etc.), diabetic nephropathy, diabetic retinopathy, diabeticneuropathy, glomerulonephritis, peptic ulcer, inflammatory bowel disease(e.g., ulcerative colitis, chronic colitis, etc.), cerebral infarction,cerebral ischemia, migraine, rheumatoid arthritis, gout, neuritis,postherpetic neuralgia, osteoarthritis, osteoporosis, systemic lupuserythematosis, rejection by organ transplantation, asthma, metastasis,Alzheimer's disease, arthritis, CNS disorders, and the like.

In order to illustrate the usefulness of the object compound (I), thepharmacological test data of the representative compound of the compound(I) are shown in the following.

Test Compounds ##STR24## Test: Assay for Inhibitory activity on theproduction of Nitric Oxide

The murine macrophage cell line RAW264.7 (American Type CultureCollection, No. TIB71) were used in this study. RAW264.7 cells weregrown on F75 plastic culture flasks at 37° C., 5% in Dulbecco's modifiedEagles medium (DMEM) supplement with L-glutamine, penicillin,streptomycin and 10% heat-inactivated fetal bovine serum. They wereremoved from culture flasks by rubber cell scraper and were centrifugedand resuspended in DMEM without phenol red. They were plated in 96-wellmicroliter plates (10⁵ cells per well) and allowed to adhere for 2hours. The test samples were added and preincubated for 1 hour.Thereafter the cells were activated by both of lipopolysaccharide (LPS)(1 μg/ml) and interferon γ (INF γ) (3 u/ml) for 18-24 hours and weremixed with an equal volume of Griess reagent (1% sulfanilamide/0.1%N-naphthylethylenediamine dihydrochloride/2.5% H₃ PO₄) and incubated atroom temperature for 10 minutes. The absorbance was read at 570 nm usingmicroplatereader and NO₂ was measured using NaNO₂ as a standard.

    ______________________________________    Test result    Test Compounds (10.sup.-5 M)                      inhibition (%)    ______________________________________    (a)               100    (b)               100    (c)               100    (d)               100    (e)               100    (f)               100    (g)               100    ______________________________________

For therapeutic administration, the object compounds (I) of the presentinvention and pharmaceutically acceptable salts thereof are used in aform of the conventional pharmaceutical preparation in admixture with aconventional pharmaceutically acceptable carrier such as an organic orinorganic solid or liquid excipient which is suitable for oral,parenteral or external administration. The pharmaceutical preparationmay be compounded in a solid form such as granule, capsule, tablet,dragee or suppository, or in a liquid form such as solution, suspensionor emulsion for injection, intravenous drip, ingestion, eye drops, etc.If needed, there may be included in the above preparation auxiliarysubstance such as stabilizing agent, wetting or emulsifying agent,buffer or any other commonly used additives.

The effective ingredient may usually be administered with a unit dose of0.001 mg/kg to 500 mg/kg, preferably 0.01 mg/kg to 10 mg/kg, 1 to 4times a day. However, the above dosage may be increased or decreasedaccording to age, weight and conditions of the patient or theadministering method.

Preferred embodiments of the object compound (I) are as follows.

W is lower alkyl, 1,2-methylenedioxyphenyl, phenyl, naphthyl, fluorenylwhich may have oxo, pyrrolyl, pyridyl, furyl, which may have phenyl,thienyl or a group of the formula: ##STR25## in which R¹ is hydrogen,halogen, lower alkyl, nitro, di(lower)alkylamino, amino, hydroxyamino orlower alkoxy,

Q is CH or N,

L is a bivalent radical selected from ##STR26## (in which Y is CH or N,Z is NH, O or S, and

--- is a single bond or a double bond) and ##STR27## (in which M is CHor N, and J is CH or N)!, A¹ is lower alkylene (more preferably C₁ -C₄alkylene; more preferably methylene), --NHCO--, ##STR28## (in which V isO or S), or --SO₂ --, T is hydrogen, phenyl or naphthyl, each of whichmay have 1 to 3 (more preferably one or two; most preferably one)substituent(s) selected from the group consisting of hydroxy, protectedhydroxy (more preferably acyloxy), halogen, lower alkoxy and loweralkyl; imidazolyl; pyridyl; indolyl; thienyl; furyl; hydroxy; loweralkanoyloxy; heterocycliccarbonyloxy(more preferablypyridylcarbonyloxy); heterocyclic(lower)alkanoyloxy (more preferablypyridyl(lower)alkanoyloxy or piperidyl(lower)alkanoyloxy);di(lower)alkylamino!(lower)alkanoyloxy; ar(lower)alkoxy (more preferablyphenyl(lower)alkoxy); sulfooxy; mercapto; lower alkylthio; mono(or di ortri)phenyl(lower)alkylthio; di(lower)-alkylamino!(lower)alkanoylthio;amino; acylamino more preferably aroylamino (more preferablybenzoylamino), lower alkanoylamino or ar(lower)alkoxycarbonylamino (morepreferably phenyl(lower)alkoxycarbonylamino)!; guanidino or guanidinohaving phenylsulfonyl substituted with 3 lower alkyl and lower alkoxy;or a group of the formula: ##STR29## (in which R² is hydroxy,phenyl(lower)alkoxy (more preferably benzyloxy); morpholinyl;piperazinyl which may have 1 to 3 (more preferably one or two; mostpreferably one) suitable substituent(s) (more preferably substituentselected from the group consisting of lower alkyl, carboxy, protectedcarboxy (more preferably esterified carboxy; most preferably loweralkoxycarbonyl), carboxy(lower)alkyl, protected carboxy(lower)alkyl(more preferably esterified carboxy(lower)alkyl; most preferably loweralkoxycarbonyl(lower)alkyl), heterocyclic group (more preferably pyridylor pyrimidinyl), cyclo(lower)alkyl, aryl (more preferably phenyl),hydroxy(lower)alkyl, protected hydroxy(lower)alkyl (more preferablyacyloxy(lower)alkyl), di(lower)alkylamino(lower)alkyl and acyl (morepreferably lower alkanoyl or lower alkoxycarbonyl); piperidyl which mayhave 1 to 3 (more preferably one or two; most preferably one) suitablesubstituent(s) (more preferably heterocyclic group; most preferablypiperidyl); pyrrolidinyl; thiomorpholinyl; homopiperazinyl which mayhave 1 to 3 (more preferably one or two; most preferably one) suitablesubstituent(s) (more preferably lower alkyl); piperazinio which may havetwo or three (more preferably two) suitable substituent (morepreferably-lower alkyl); piperidyloxy which may have 1 to 3 (morepreferably one or two; most preferably one) suitable substituent(s)(more preferably lower alkyl); or amino having one or two substituent(s)selected from the group consisting of lower alkyl, ar(lower)alkyl (morepreferably phenyl(lower)alkyl), cyclo(lower)alkyl, heterocyclic group(more preferably morpholinyl or pyrazolyl), mono (or di ortri)hydroxy(lower)alkyl (more preferably di(or tri)hydroxyklower)alkyl),mono(or di or tri)(protected hydroxy)(lower)alkyl (more preferably di(ortri)acyloxy(lower)alkyl) and di(lower)alkylamino!(lower)alkyl morepreferably mono(or di)(lower)alkylamino, cyclo(lower)alkylamino,phenyl(lower)alkylamino, morpholinylamino, pyrazolylamino,di(lower)alkylamino!(lower)alkylamino, amino having lower alkyl anddi(lower)alkylamino!(lower)alkyl, di(or tri)hydroxy(lower)alkylamino!;

A² is lower alkylene (more preferably C₁ -C₂ alkylene),

R⁸ is hydrogen or lower alkyl, or

R⁸ and a group of the formula: --A² --T are linked together to form agroup of the formula: ##STR30## R³ is hydrogen; phenyl which may have 1to 3 (more preferably one or two; most preferably one) suitablesubstituent(s) more preferably substituent selected from the groupconsisting of hydroxy, protected hydroxy (more preferablyphenyl(lower)alkoxy), lower alkoxy and halogen!; hydroxy; protectedhydroxy (more preferably acyloxy); cyclo(lower)alkyl; lower alkylthio;pyridyl; imidazolyl which may have acyl (more preferably tolylsulfonyl);thienyl; or furyl;

A³ is bond or lower alkylene,

R⁹ is hydrogen or lower alkyl, or

R⁹ and a group of the formula: --A³ --R³ are linked together to form agroup of the formula: ##STR31## R⁴ is carboxy, esterified carboxy (morepreferably lower alkoxycarbonyl), piperazinylcarbonyl which may havelower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula:##STR32## (in which R⁵ is hydrogen or lower alkyl, and

R⁶ is hydrogen; phenyl; phenyl(lower)alkyl which may have 1 to 3 (morepreferably one or two; most preferably one) suitable substituent(s)(more preferably substituent selected from the group consisting of loweralkyl, lower alkoxy, carboxy, protected carboxy (more preferablyesterified carboxy; most preferably lower alkoxycarbonyl), mono(or di ortri)halo(lower)alkyl (more preferably trihalo(lower)alkyl),di(lower)alkylamino, di(lower)alkylamino!(lower)alkyl,di(lower)alkylamino!(lower)alkoxy, halogen and heterocyclic group (morepreferably triazolyl, piperazinyl, pyrazolyl or imidazolyl) which mayhave lower alkyl); di(lower)alkylamino!(lower)alkyl; pyridyl(lower)alkylwhich may have 1 to 3 (more preferably one or two; most preferably one)suitable substituent(s) (more preferably substituent selected from thegroup consisting of lower alkyl, lower alkoxy, halogen,di(lower)alkylamino, protected amino (more preferably acylamino; loweralkanoylamino), heterocyclic group (more preferably pyridyl) and loweralkylthio), quinolyl(lower)alkyl, quinoxalinyl(lower)alkyl,pyrimidinyl(lower)alkyl, pyrazinyl(lower)alkyl, pyrazolyl(lower)alkyl orbenzimidazolyl(lower)alkyl), or

R⁴ and a group of the formula: --A³ --R³ are linked together to form##STR33## (in which R¹⁰ is phenyl(lower)alkyl), with proviso that

when M is CH, and J is CH, then Q is N.

More preferred embodiment(s) of the object compound (I) are representedby the following formulae (A)˜(D). ##STR34## wherein W is lower alkyl,1,2-methylenedioxyphenyl, phenyl, naphthyl, fluorenyl which may haveoxo, pyrrolyl, pyridyl, furyl which may have phenyl, thienyl or a groupof the formula: ##STR35## in which R¹ is hydrogen, halogen, lower alkyl,nitro, di(lower)alkylamino, amino, hydroxyamino or lower alkoxy,

Q is CH or N,

L is a bivalent radical selected from ##STR36## (in which Y is CH or N,Z is NH, O or S, and

--- is a single bond or a double bond) and ##STR37## (in which M is CHor N, and J is CH or N)!,

A¹ is lower alkylene (more preferably C₁ -C₄ alkylene;

more preferably methylene), --NHCO--, ##STR38## (in which V is O or S),or --SO₂ --, R² is morpholinyl,

A² is lower alkylene (more preferably C₁ -C₂ alkylene),

R⁸ is hydrogen or lower alkyl,

R³ is hydrogen; phenyl which may have 1 to 3 (more preferably one ortwo; most preferably one) suitable substituent(s) more preferablysubstituent selected from the group consisting of hydroxy, protectedhydroxy (more preferably phenyl(lower)alkoxy), lower alkoxy andhalogen!; hydroxy; protected hydroxy (more preferably acyloxy);cyclo(lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may haveacyl (more preferably tolylsulfonyl); thienyl; or furyl;

A³ is bond or lower alkylene,

R⁹ is hydrogen or lower alkyl, or

R⁹ and a group of the formula: --A³ --R³ are linked together to form agroup of the formula: ##STR39## R⁴ is carboxy, esterified carboxy (morepreferably lower alkoxycarbonyl), piperazinylcarbonyl which may havelower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula:##STR40## (in which R⁵ is hydrogen or lower alkyl, and

R⁶ is hydrogen; phenyl; pyridyl(lower)alkyl substituted with 1 to 3(more preferably one or two; most preferably one) suitablesubstituent(s) (more preferably substituent selected from the groupconsisting of lower alkyl, lower alkoxy, halogen, di(lower)alkylamino,protected amino (more preferably acylamino; lower alkanoylamino),heterocyclic group (more preferably pyridyl) and lower alkylthio),quinolyl(lower)alkyl, quinoxalinyl(lower)alkyl, pyrimidinyl(lower)alkyl,pyrazinyl(lower)alkyl, pyrazolyl (lower)alkyl orbenzimidazolyl(lower)alkyl), or

R⁴ and a group of the formula: --A³ --R³ are linked together to form##STR41## (in which R¹⁰ is phenyl(lower)alkyl), with proviso that when Mis CH, and J is CH, then Q is N. ##STR42## wherein W is lower alkyl,1,2-methylenedioxyphenyl, phenyl, naphthyl, fluorenyl which may haveoxo, pyrrolyl, pyridyl, furyl which may have phenyl, thienyl or a groupof the formula: ##STR43## in which R¹ is hydrogen, halogen, lower alkyl,nitro, di(lower)alkylamino, amino, hydroxyamino or lower alkoxy,

Q is CH or N,

L is a bivalent radical selected from ##STR44## (in which Y is CH or N,Z is NH, O or S, and

--- is a single bond or a double bond) and ##STR45## (in which M is CHor N, and J is CH or N)!,

A¹ is lower alkylene (more preferably C₁ -C₄ alkylene; more preferablymethylene), --NHCO--, ##STR46## (in which V is O or S), or --SO₂ --, R²is lower alkylpiperazinyl,

A² is lower alkylene (more preferably C₁ -C₂ alkylene),

R⁸ is hydrogen or lower alkyl,

R³ is hydrogen; phenyl which may have 1 to 3 (more preferably one ortwo; most preferably one) suitable substituent(s) more preferablysubstituent selected from the group consisting of hydroxy, protectedhydroxy (more preferably phenyl(lower)alkoxy), lower alkoxy andhalogen!; hydroxy; protected hydroxy (more preferably acyloxy);cyclo(lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may haveacyl (more preferably tolylsulfonyl); thienyl; or furyl;

A³ is bond or lower alkylene,

R⁹ is hydrogen or lower alkyl, or

R⁹ and a group of the formula: --A³ --R³ are linked together to form agroup of the formula: ##STR47## R⁴ is carboxy, esterified carboxy (morepreferably lower alkoxycarbonyl), piperazinylcarbonyl which may havelower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula:##STR48## (in which R⁵ is hydrogen or lower alkyl, and

R⁶ is hydrogen; phenyl; phenyl(lower)alkyl which may have 1 to 3 (morepreferably one or two; most preferably one) suitable substituent(s)(more preferably substituent selected from the group consisting of loweralkyl, lower alkoxy, carboxy, protected carboxy (more preferablyesterified carboxy; most preferably lower alkoxycarbonyl), mono(or di ortri)halo(lower)alkyl (more preferably trihalo(lower)alkyl),di(lower)alkylamino, di(lower)alkylamino!(lower)alkyl,di(lower)-alkylamino!(lower)alkoxy, halogen and heterocyclic group (morepreferably triazolyl, piperazinyl, pyrazolyl or imidazolyl) which mayhave lower alkyl); di(lower)alkylamino!(lower)alkyl; pyridyl(lower)alkylwhich may have 1 to 3 (more preferably one or two; most preferably one)suitable substituent(s) (more preferably substituent selected from thegroup consisting of lower alkyl, lower alkoxy, halogen,di(lower)alkylamino, protected amino (more preferably acylamino; loweralkanoylamino), heterocyclic group (more preferably pyridyl) and loweralkylthio), quinolyl(lower)alkyl, quinoxalinyl(lower)alkyl,pyrimidinyl(lower)alkyl, pyrazinyl(lower)alkyl, pyrazolyl(lower)alkyl orbenzimidazolyl(lower)alkyl), or

R⁴ and a group of the formula: --A³ --R³ are linked together to form##STR49## (in which R¹⁰ is phenyl(lower)alkyl), with proviso that

when M is CH, and J is CH, then Q is N. ##STR50## wherein W is loweralkyl, 1,2-methylenedioxyphenyl, phenyl, naphthyl, fluorenyl which mayhave oxo, pyrrolyl, pyridyl, furyl which may have phenyl, thienyl or agroup of the formula: ##STR51## in which R¹ is hydrogen, halogen, loweralkyl, nitro, di(lower)alkylamino, amino, hydroxyamino or lower alkoxy,

Q is CH or N,

L is a bivalent radical selected from ##STR52## (in which Y is CH or N,Z is NH, O or S, and --- is a single bond or a double bond) and##STR53## (in which M is CH or N, and J is CH or N)!, A¹ is loweralkylene (more preferably C₁ -C₄ alkylene;

more preferably methylene), --NHCO--, ##STR54## (in which V is O or S),or --SO₂ --, A² is lower alkylene (more preferably C₁ -C₂ alkylene),

R⁸ is hydrogen or lower alkyl,

R³ is hydrogen; phenyl which may have 1 to 3 (more preferably one ortwo; most preferably one) suitable substituent(s) more preferablysubstituent selected from the group consisting of hydroxy, protectedhydroxy (more preferably phenyl(lower)alkoxy), lower alkoxy andhalogen!; hydroxy; protected hydroxy (more preferably acyloxy);cyclo(lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may haveacyl (more preferably tolylsulfonyl); thienyl; or furyl;

A³ is bond or lower alkylene,

R⁹ is hydrogen or lower alkyl, or

R⁹ and a group of the formula: --A³ --R³ are linked together to form agroup of the formula: ##STR55## R⁴ is carboxy, esterified carboxy (morepreferably lower alkoxycarbonyl), piperazinylcarbonyl which may havelower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula:##STR56## (in which R⁵ is hydrogen or lower alkyl, and

R⁶ is hydrogen; phenyl; phenyl(lower)alkyl which may have 1 to 3 (morepreferably one or two; most preferably one) suitable substituent(s)(more preferably substituent selected from the group consisting of loweralkyl, lower alkoxy, carboxy, protected carboxy (more preferablyesterified carboxy; most preferably lower alkoxycarbonyl), mono(or di ortri)halo(lower)alkyl (more preferably trihalo(lower)alkyl),di(lower)alkylamino, di(lower)alkylamino!(lower)alkyl,di(lower)alkylamino!(lower)alkoxy, halogen and heterocyclic group (morepreferably triazolyl, piperazinyl, pyrazolyl or imidazolyl) which mayhave lower alkyl); di(lower) alkylamino!(lower)alkyl;pyridyl(lower)alkyl which may have 1 to 3 (more preferably one or two;most preferably one) suitable substituent(s) (more preferablysubstituent selected from the group consisting of lower alkyl, loweralkoxy, halogen, di(lower)alkylamino, protected amino (more preferablyacylamino; lower alkanoylamino), heterocyclic group (more preferablypyridyl) and lower alkylthio), quinolyl(lower)alkyl,quinoxalinyl(lower)alkyl, pyrimidinyl(lower)alkyl,pyrazinyl(lower)alkyl, pyrazolyl(lower)alkyl orbenzimidazolyl(lower)alkyl), or

R⁴ and a group of the formula: --A³ --R³ are linked together to form##STR57## (in which R¹⁰ is phenyl(lower)alkyl), with proviso that

when M is CH, and J is CH, then Q is N. ##STR58## wherein W is loweralkyl, 1,2-methylenedioxyphenyl, phenyl, naphthyl, fluorenyl which mayhave oxo, pyrrolyl, pyridyl, furyl which may have phenyl, thienyl or agroup of the formula: ##STR59## in which R¹ is hydrogen, halogen, loweralkyl, nitro, di(lower)alkylamino, amino, hydroxyamino or lower alkoxy,

Q is CH or N,

L is a bivalent radical selected from ##STR60## (in which Y is CH or N,Z is NH, O or S, and

--- is a single bond or a double bond) and ##STR61## (in which M is CHor N, and J is CH or N)!, A¹ is lower alkylene (more preferably C₁ -C₄alkylene;

more preferably methylene), --NHCO--, ##STR62## (in which V is O or S),or --SO₂ --, T is hydroxy or lower alkylthio,

A² is lower alkylene (more preferably C₁ -C₂ alkylene),

R⁸ is hydrogen or lower alkyl,

R³ is hydrogen; phenyl which may have 1 to 3 (more preferably one ortwo; most preferably one) suitable substituent(s) more preferablysubstituent selected from the group consisting of hydroxy, protectedhydroxy (more preferably phenyl(lower)alkoxy), lower alkoxy andhalogen!; hydroxy; protected hydroxy (more preferably acyloxy);cyclo(lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may haveacyl (more preferably tolylsulfonyl); thienyl; or furyl;

A³ is bond or lower alkylene,

R⁹ is hydrogen or lower alkyl, or

R⁹ and a group of the formula: --A³ --R³ are linked together to form agroup of the formula: ##STR63## R⁴ is carboxy, esterified carboxy (morepreferably lower alkoxycarbonyl), piperazinylcarbonyl which may havelower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula:##STR64## (in which R⁵ is hydrogen or lower alkyl, and

R⁶ is hydrogen; phenyl; di(lower)alkylamino!(lower)alkyl;pyridyl(lower)alkyl substituted with 1 to 3 (more preferably one or two;most preferably one) suitable substituent(s) (more preferablysubstituent selected from the group consisting of lower alkyl, loweralkoxy, halogen, di(lower)alkylamino, protected amino (more preferablyacylamino; lower alkanoylamino), heterocyclic group (more preferablypyridyl) and lower alkylthio), quinolyl(lower)alkyl,quinoxalinyl(lower)alkyl, pyrimidinyl(lower)alkyl,pyrazinyl(lower)alkyl, pyrazolyl(lower)alkyl orbenzimidazolyl(lower)alkyl), or

R⁴ and a group of the formula: --A³ --R³ are linked together to form##STR65## (in which R¹⁰ is phenyl(lower)alkyl), with proviso that

when M is CH, and J is CH, then Q is N.

The following Preparations and Examples are given for the purpose ofillustrating the present invention in detail.

In the following Examples and Preparations, there are employed the otherabbreviations in addition to the abbreviations adopted by the IUPAC-IUB(Commission on Biological Nomenclature).

The abbreviations used are as follows.

    ______________________________________    Ac               acetyl    1 #STR66##       3-cyclohexyl-L-alanine    2 #STR67##       3-(2-furyl)-L-alanine    3 #STR68##       3-(3-furyl)-L-alanine    4 #STR69##       3-(2-thienyl)-L-alanine    Arg              L-arginine    Asp              L-aspartic acid    D-Asp            D-aspartic acid    Boc              t-butoxycarbonyl    Bz               benzoyl    Bzl              benzyl    Bzl(4-COOH)      4-carboxybenzyl    Bzl(4-COOMe)     4-methoxycarbonylbenzyl    Bzl(4-OH)        4-hydroxybenzyl    Bzl(4-NMe.sub.2) 4-dimethylaminobenzyl    Bzl(4-CH.sub.2 NMe.sub.2)                     4-(dimethylaminomethyl)benzyl    Bzl(4-Cl)        4-chlorobenzyl    Bzl(4-Br)        4-bromobenzyl    Bzl(4-F)         4-fluorobenzyl    Bzl(4-OMe)       4-methoxybenzyl    Bzl(2-Me)        2-methylbenzyl    Bzl(3-Me)        3-methylbenzyl    Bzl(4-Me)        4-methylbenzyl    Bzl(4-CF.sub.3)  4-trifluoromethylbenzyl    Bzl(4-O--(CH.sub.2).sub.2 --NMe.sub.2)                     4-(2-dimethylaminoethoxy)benzyl    5 #STR70##       4-(1-1H-imidazolyl)benzyl    6 #STR71##       4-(1-methylpiperazin-4-yl)benzyl    7 #STR72##       4-(1-methylpyrazol-3-yl)benzyl    8 #STR73##       4-(1-1H-triazolyl)benzyl    Cys              L-cysteine    Et               ethyl    Glu              L-glutamic acid    Gly              glycine    His              L-histidine    Leu              L-leucine    Lys              L-lysine    Me               methyl    MePhe            N-methyl-L-phenylalanine    Met              L-methionine    1Nal             3-(1-naphthyl)-L-alanine    2Nal             3-(2-naphthyl)-L-alanine    1Naph            1-naphthyl    2Naph            2-naphthyl    Nle              L-norleucine    Nva              L-norvaline    Orn              L-ornithine    .sup.n Pr        n-propyl    Phe              L-phenylalanine    D-Phe            D-phenylalanine    Phe(4-Cl)        3-(4-chlorophenyl)-L-alanine    Phe(4-Me)        3-(4-methylphenyl)-L-alanine    Phg              (S)-2-phenylglycine    4Pm              4-Pyrimidinyl    2Pyala           3-(2-pyridyl)-L-alanine    3Pyala           3-(3-pyridyl)-L-alanine    4Pyala           3-(4-pyridyl)-L-alanine    2Py              2-pyridyl    3Py              3-pyridyl    4Py              4-pyridyl    3Py(6-NHAc)      (6-acetylaminopyridin-3-yl)    3Py(5-Br)        (5-bromopyridin-3-yl)    3Py(6-Cl)        (6-chloropyridin-3-yl)    3Py(6-NMe.sub.2) (6-dimethylaminopyridin-3-yl)    3Py(6-OEt)       (6-ethoxypyridin-3-yl)    3Py(4-OMe)       (4-methoxypyridin-3-yl)    3Py(5-OMe)       (5-methoxypyridin-3-yl)    3Py(6-OMe)       (6-methoxypyridin-3-yl)    3Py(6-Me)        (6-methoxypyridin-3-yl)    3Py(6-SMe)       (6-methylthiopyridin-3-yl)    3Py(6-n-Pr       (6-n-propylpyridin-3-yl)    3Py(6-2Py)        6-(2-pyridyl)pyridin-3-yl!    3Py(6-3Py)        6-(3-pyridyl)pyridin-3-yl!    2Qu              2-quinolyl    3Qu              3-quinolyl    6Qu              6-quinolyl    7Qu              7-quinolyl    Ser              L-serine    Thr              L-trheonine    Tos              p-toluenesulfonyl    Trt              trityl    Tyr              L-tyrosine    Val              L-valine    Z                benzyloxycarbonyl    Z(2-Cl)          2-chlorobenzyloxycarbonyl    ______________________________________

The Starting Compounds used and the Object Compounds obtained in thefollowing Prenarations and Examples are given in the Table as below, inwhich the formulae of the Starting Compounds are in the upper and theformulae of the Object Compounds are in the lower, respectively.

                                      TABLE    __________________________________________________________________________    Preparation No.           Formula    __________________________________________________________________________     1           1 #STR74##           2 #STR75##     2           1 #STR76##           3 #STR77##     3           2 #STR78##           4 #STR79##     4           5 #STR80##           6 #STR81##     5-(1)           3 #STR82##           7 #STR83##     5-(2)           8 #STR84##           9 #STR85##     5-(3)           0 #STR86##           1 #STR87##     5-(4)           2 #STR88##           3 #STR89##     5-(5)           4 #STR90##           5 #STR91##     5-(6)           6 #STR92##           7 #STR93##     5-(7)           8 #STR94##           9 #STR95##     6           9 #STR96##           0 #STR97##     7           8 #STR98##           1 #STR99##     8           2 #STR100##           3 #STR101##     9-(1)           4 #STR102##           5 #STR103##     9-(2)           6 #STR104##           7 #STR105##     10           8 #STR106##           9 #STR107##     11           7 #STR108##           0 #STR109##     12-(1)           6 #STR110##           4 #STR111##     12-(2)           5 #STR112##           6 #STR113##     12-(3)           5 #STR114##           1 #STR115##     12-(4)           2 #STR116##           3 #STR117##     13           1 #STR118##           2 #STR119##     14-(1)           9 #STR120##           5 #STR121##     14-(2)           2 #STR122##           2 #STR123##     14-(3)           2 #STR124##           0 #STR125##     14-(4)           2 #STR126##           4 #STR127##     14-(5)           2 #STR128##           6 #STR129##     14-(6)           4 #STR130##           8 #STR131##     15           5 #STR132##           6 #STR133##     16           6 #STR134##           7 #STR135##     17           0 #STR136##           8 #STR137##     18-(1)           3 #STR138##           9 #STR139##     18-(2)           1 #STR140##           0 #STR141##     19           5 #STR142##           1 #STR143##     20           2 #STR144##           3 #STR145##     21           4 #STR146##           5 #STR147##     22           5 #STR148##           6 #STR149##     23           7 #STR150##           8 #STR151##     24           9 #STR152##           0 #STR153##     25           1 #STR154##           2 #STR155##     26           3 #STR156##           4 #STR157##     27           5 #STR158##           6 #STR159##     28           4 #STR160##           7 #STR161##     29           6 #STR162##           8 #STR163##     30           9 #STR164##           5 #STR165##     31           0 #STR166##           1 #STR167##     32           1 #STR168##           2 #STR169##     33           2 #STR170##           3 #STR171##     34           9 #STR172##           4 #STR173##     35           4 #STR174##           5 #STR175##     36           8 #STR176##           6 #STR177##     37           7 #STR178##           8 #STR179##     38           9 #STR180##           0 #STR181##     39-(1)           5 #STR182##           1 #STR183##     39-(2)           7 #STR184##           4 #STR185##     39-(3)           5 #STR186##           2 #STR187##     39-(4)           5 #STR188##           3 #STR189##     39-(5)           4 #STR190##           5 #STR191##     39-(6)           5 #STR192##           6 #STR193##     39-(7)           5 #STR194##           7 #STR195##     39-(8)           5 #STR196##           8 #STR197##     39-(9)           5 #STR198##           9 #STR199##     39-(10)           5 #STR200##           0 #STR201##     39-(11)           5 #STR202##           1 #STR203##     39-12)           5 #STR204##           2 #STR205##     39-(13)           5 #STR206##           3 #STR207##     39-(14)           5 #STR208##           8 #STR209##     39-(15)           5 #STR210##           9 #STR211##     39-(16)           5 #STR212##           0 #STR213##     39-(17)           5 #STR214##           1 #STR215##     39-(18)           5 #STR216##           2 #STR217##     39-(19)           5 #STR218##           3 #STR219##     39-(20)           5 #STR220##           4 #STR221##     39-(21)           5 #STR222##           5 #STR223##     39-(22)           5 #STR224##           6 #STR225##     39-(23)           5 #STR226##           3 #STR227##     39-(24)           5 #STR228##           7 #STR229##     39-(25)           1 #STR230##           8 #STR231##     39-(26)           2 #STR232##           9 #STR233##     39-(27)           5 #STR234##           0 #STR235##     39-(28)           3 #STR236##           1 #STR237##     40           3 #STR238##           3 #STR239##     41           0 #STR240##           4 #STR241##     42-(1)           1 #STR242##           5 #STR243##     42-(2)           6 #STR244##           7 #STR245##     42-(3)           8 #STR246##           9 #STR247##     42-(4)           0 #STR248##           1 #STR249##     42-(5)           2 #STR250##           3 #STR251##     42-(6)           4 #STR252##           5 #STR253##     42-(7)           6 #STR254##           7 #STR255##     42-(8)           8 #STR256##           8 #STR257##     42-(9)           9 #STR258##           9 #STR259##     42-(10)           0 #STR260##           0 #STR261##     42-(11)           1 #STR262##           1 #STR263##     42-(12)           2 #STR264##           2 #STR265##     42-(13)           2 #STR266##           3 #STR267##     42-(14)           6 #STR268##           4 #STR269##     42-(15)           3 #STR270##           5 #STR271##     42-(16)           7 #STR272##           6 #STR273##     42-(17)           8 #STR274##           7 #STR275##     42-(18)           9 #STR276##           8 #STR277##     42-(19)           0 #STR278##           9 #STR279##     42-(20)           1 #STR280##           0 #STR281##     43-(1)           1 #STR282##           2 #STR283##     43-(2)           3 #STR284##           4 #STR285##     44           1 #STR286##           5 #STR287##     45-(1)           6 #STR288##           7 #STR289##     45-(2)           8 #STR290##           9 #STR291##     45-(3)           1 #STR292##           0 #STR293##     46-(1)           2 #STR294##           1 #STR295##     46-(2)           9 #STR296##           2 #STR297##     46-(3)           2 #STR298##           3 #STR299##     46-(4)           9 #STR300##           4 #STR301##     46-(5)           9 #STR302##           5 #STR303##     46-(6)           9 #STR304##           6 #STR305##     46-(7)           9 #STR306##           7 #STR307##     46-(8)           9 #STR308##           8 #STR309##     46-(9)           5 #STR310##           6 #STR311##     46-(10)           5 #STR312##           7 #STR313##     46-(11)           9 #STR314##           9 #STR315##     46-(12)           9 #STR316##           0 #STR317##     46-(13)           9 #STR318##           1 #STR319##     46-(14)           2 #STR320##           2 #STR321##     46-(15)           9 #STR322##           3 #STR323##     46-(16)           9 #STR324##           4 #STR325##     46-(17)           2 #STR326##           5 #STR327##     46-(18)           2 #STR328##           6 #STR329##     46-(19)           9 #STR330##           7 #STR331##     46-(20)           9 #STR332##           8 #STR333##     46-(21)           9 #STR334##           9 #STR335##     46-(22)           9 #STR336##           0 #STR337##     46-(23)           9 #STR338##           1 #STR339##     46-(24)           9 #STR340##           2 #STR341##     46-(25)           9 #STR342##           3 #STR343##     46-(26)           4 #STR344##           1 #STR345##     46-(27)           4 #STR346##           3 #STR347##     47           4 #STR348##           Compound A           2 #STR349##           5 #STR350##     48           6 #STR351##           6 #STR352##     49           7 #STR353##           Compound A           2 #STR354##           8 #STR355##     50-(1)           9 #STR356##           0 #STR357##     50-(2)           1 #STR358##           2 #STR359##     50-(3)           3 #STR360##           4 #STR361##     50-(4)           3 #STR362##           5 #STR363##     50-(5)           6 #STR364##           7 #STR365##     50-(6)           8 #STR366##           9 #STR367##     50-(7)           0 #STR368##           1 #STR369##     50-(8)           2 #STR370##           3 #STR371##     50-(9)           4 #STR372##           5 #STR373##     50-(10)           6 #STR374##           7 #STR375##     50-(11)           8 #STR376##           9 #STR377##     50-(12)           0 #STR378##           1 #STR379##     50-(13)           0 #STR380##           0 #STR381##     50-(14)           2 #STR382##           3 #STR383##     51-(1)           4 #STR384##           5 #STR385##     51-(2)           6 #STR386##           7 #STR387##     51-(3)           5 #STR388##           9 #STR389##     51-(4)           6 #STR390##           8 #STR391##     51-(5)           7 #STR392##           0 #STR393##     51-(6)           8 #STR394##           1 #STR395##     51-(7)           2 #STR396##           3 #STR397##     51-(8)           4 #STR398##           5 #STR399##     51-(9)           9 #STR400##           6 #STR401##     51-(10)           0 #STR402##           7 #STR403##     51-(11)           1 #STR404##           8 #STR405##     51-(12)           2 #STR406##           0 #STR407##     51-(13)           3 #STR408##           1 #STR409##     51-(14)           4 #STR410##           2 #STR411##     51-(15)           5 #STR412##           3 #STR413##     51-(16)           6 #STR414##           4 #STR415##     51-(17)           7 #STR416##           5 #STR417##     51-(18)           6 #STR418##           7 #STR419##     51-(19)           8 #STR420##           8 #STR421##     51-(20)           9 #STR422##           9 #STR423##     51-(21)           0 #STR424##           0 #STR425##     51-(22)           1 #STR426##           1 #STR427##     51-(23)           2 #STR428##           2 #STR429##     51-(24)           3 #STR430##           3 #STR431##     51-(25)           4 #STR432##           5 #STR433##     51-(26)           6 #STR434##           7 #STR435##     51-(27)           8 #STR436##           9 #STR437##     51-(28)           1 #STR438##           1 #STR439##     51-(29)           0 #STR440##           2 #STR441##     52           5 #STR442##           3 #STR443##     53-(1)           5 #STR444##           4 #STR445##     53-(2)           5 #STR446##           5 #STR447##     54           6 #STR448##           7 #STR449##     55           8 #STR450##           9 #STR451##     56           7 #STR452##           1 #STR453##     57-(1)           2 #STR454##           3 #STR455##     57-(2)           2 #STR456##           5 #STR457##     57-(3)           6 #STR458##           7 #STR459##     57-(4)           8 #STR460##           9 #STR461##     57-(5)           2 #STR462##           1 #STR463##     58-(1)           9 #STR464##           3 #STR465##     58-(2)           1 #STR466##           5 #STR467##     58-(3)           7 #STR468##           6 #STR469##     58-(4)           5 #STR470##           7 #STR471##     58-(5)           3 #STR472##           8 #STR473##     58-(6)           1 #STR474##           0 #STR475##     59           1 #STR476##           2 #STR477##     60-(1)           3 #STR478##           4 #STR479##     60-(2)           5 #STR480##           2 #STR481##     60-(3)           7 #STR482##           8 #STR483##     60-(4)           9 #STR484##           0 #STR485##     60-(5)           1 #STR486##           2 #STR487##     60-(6)           3 #STR488##           4 #STR489##     60-(7)           9 #STR490##           6 #STR491##     60-(8)           9 #STR492##           5 #STR493##     60-(9)           7 #STR494##           8 #STR495##     60-(10)           5 #STR496##           9 #STR497##     60-(11)           5 #STR498##           0 #STR499##     60-(12)           1 #STR500##           2 #STR501##     60-(13)           5 #STR502##           3 #STR503##     60-(14)           5 #STR504##           4 #STR505##     60-(15)           5 #STR506##           6 #STR507##     60-(16)           5 #STR508##           7 #STR509##     60-(17)           8 #STR510##           9 #STR511##     60-(18)           0 #STR512##           1 #STR513##     60-(19)           0 #STR514##           2 #STR515##     60-(20)           0 #STR516##           3 #STR517##     60-(21)           4 #STR518##           5 #STR519##     60-(22)           6 #STR520##           7 #STR521##     60-(23)           6 #STR522##           8 #STR523##     60-(24)           9 #STR524##           9 #STR525##     60-(25)           3 #STR526##           0 #STR527##     60-(26)           3 #STR528##           1 #STR529##     60-(27)           2 #STR530##           2 #STR531##     60-(28)           5 #STR532##           3 #STR533##     60-(29)           3 #STR534##           4 #STR535##     60-(30)           8 #STR536##           5 #STR537##     60-(31)           0 #STR538##           6 #STR539##     60-(32)           6 #STR540##           7 #STR541##     60-(33)           5 #STR542##           8 #STR543##     60-(34)           9 #STR544##           0 #STR545##     60-(35)           1 #STR546##           2 #STR547##     60-(36)           5 #STR548##           3 #STR549##     60-(37)           5 #STR550##           4 #STR551##     60-(38)           5 #STR552##           6 #STR553##     60-(39)           1 #STR554##           7 #STR555##     60-(40)           8 #STR556##           9 #STR557##     60-(41)           5 #STR558##           0 #STR559##     60-(42)           1 #STR560##           2 #STR561##     60-(43)           5 #STR562##           3 #STR563##     60-(44)           4 #STR564##           5 #STR565##     60-(45)           6 #STR566##           7 #STR567##     60-(46)           5 #STR568##           8 #STR569##     60-(47)           5 #STR570##           9 #STR571##     60-(48)           5 #STR572##           0 #STR573##     61-(1)           1 #STR574##           2 #STR575##     61-(2)           4 #STR576##           3 #STR577##     61-(3)           4 #STR578##           5 #STR579##     61-(4)           6 #STR580##           7 #STR581##     61-(5)           8 #STR582##           9 #STR583##     61-(6)           0 #STR584##           1 #STR585##     61-(7)           2 #STR586##           3 #STR587##     61-(8)           4 #STR588##           5 #STR589##     61-(9)           6 #STR590##           7 #STR591##     61-(10)           8 #STR592##           9 #STR593##     61-(11)           9 #STR594##           0 #STR595##     61-(12)           1 #STR596##           2 #STR597##     61-(13)           3 #STR598##           4 #STR599##     61-(14)           5 #STR600##           6 #STR601##     61-(15)           7 #STR602##           8 #STR603##     61-(16)           9 #STR604##           0 #STR605##     61-(17)           7 #STR606##           1 #STR607##     61-(18)           9 #STR608##           2 #STR609##     61-(19)           1 #STR610##           3 #STR611##     61-(20)           2 #STR612##           4 #STR613##     61-(21)           5 #STR614##           6 #STR615##     61-(22)           5 #STR616##           7 #STR617##     61-(23)           7 #STR618##           8 #STR619##     61-(24)           8 #STR620##           9 #STR621##     61-(25)           0 #STR622##           1 #STR623##     61-(26)           2 #STR624##           3 #STR625##     61-(27)           4 #STR626##           5 #STR627##     61-(28)           2 #STR628##           6 #STR629##     61-(29)           7 #STR630##           8 #STR631##     61-(30)           9 #STR632##           0 #STR633##     61-(31)           1 #STR634##           2 #STR635##     61-(32)           6 #STR636##           4 #STR637##     61-(33)           7 #STR638##           6 #STR639##     61-(34)           8 #STR640##           3 #STR641##     61-(35)           0 #STR642##           5 #STR643##     61-(36)           2 #STR644##           0 #STR645##     61-(37)           7 #STR646##           8 #STR647##     61-(38)           9 #STR648##           0 #STR649##     61-(39)           6 #STR650##           1 #STR651##     61-(40)           2 #STR652##           3 #STR653##     61-(41)           9 #STR654##           4 #STR655##     61-(42)           0 #STR656##           5 #STR657##     61-(43)           2 #STR658##           6 #STR659##     61-(44)           7 #STR660##           8 #STR661##     61-(45)           5 #STR662##           9 #STR663##     61-(46)           7 #STR664##           0 #STR665##     61-(47)           8 #STR666##           1 #STR667##     61-(48)           9 #STR668##           2 #STR669##     61-(49)           0 #STR670##           3 #STR671##     62-(1)           4 #STR672##           5 #STR673##     62-(2)           7 #STR674##           8 #STR675##     62-(3)           9 #STR676##           0 #STR677##     63-(1)           1 #STR678##           6 #STR679##     63-(2)           2 #STR680##           7 #STR681##     63-(3)           8 #STR682##           9 #STR683##     63-(4)           5 #STR684##           0 #STR685##     63-(5)           5 #STR686##           1 #STR687##     63-(6)           5 #STR688##           2 #STR689##     63-(7)           5 #STR690##           3 #STR691##     63-(8)           5 #STR692##           4 #STR693##     63-(9)           5 #STR694##           5 #STR695##     63-(10)           5 #STR696##           6 #STR697##     63-(11)           5 #STR698##           7 #STR699##     63-(12)           5 #STR700##           8 #STR701##     63-(13)           3 #STR702##           9 #STR703##     63-(14)           0 #STR704##           1 #STR705##     63-(15)           5 #STR706##           2 #STR707##     63-(16)           4 #STR708##           3 #STR709##     63-(17)           5 #STR710##           4 #STR711##     63-(18)           5 #STR712##           5 #STR713##     63-(19)           5 #STR714##           6 #STR715##     63-(20)           5 #STR716##           7 #STR717##     63-(21)           5 #STR718##           8 #STR719##     63-(22)           5 #STR720##           9 #STR721##     63-(23)           5 #STR722##           0 #STR723##     63-(24)           1 #STR724##           2 #STR725##     63-(25)           5 #STR726##           3 #STR727##     63-(26)           5 #STR728##           4 #STR729##     63-(27)           5 #STR730##           6 #STR731##     63-(28)           5 #STR732##           7 #STR733##     63-(29)           6 #STR734##           8 #STR735##     64-(5)           9 #STR736##           0 #STR737##     64-(6)           2 #STR738##           1 #STR739##     64-(7)           2 #STR740##           3 #STR741##     64-(8)           4 #STR742##           4 #STR743##     64-(9)           5 #STR744##           5 #STR745##     64-(10)           6 #STR746##           6 #STR747##     64-(11)           7 #STR748##           7 #STR749##     64-(12)           8 #STR750##           8 #STR751##     64-(13)           9 #STR752##           9 #STR753##     64-(14)           0 #STR754##           1 #STR755##     64-(15)           2 #STR756##           3 #STR757##     64-(16)           4 #STR758##           5 #STR759##     64-(17)           4 #STR760##           6 #STR761##     64-(18)           5 #STR762##           7 #STR763##     64-(19)           6 #STR764##           8 #STR765##     64-(20)           9 #STR766##           0 #STR767##     64-(21)           1 #STR768##           2 #STR769##     64-(22)           8 #STR770##           3 #STR771##     64-(23)           9 #STR772##           4 #STR773##     64-(24)           0 #STR774##           5 #STR775##     64-(25)           1 #STR776##           6 #STR777##     64-(26)           7 #STR778##           8 #STR779##     64-(27)           4 #STR780##           9 #STR781##     64-(28)           0 #STR782##           1 #STR783##     64-(29)           2 #STR784##           2 #STR785##     64-(30)           8 #STR786##           3 #STR787##     64-(31)           4 #STR788##           5 #STR789##     64-(32)           6 #STR790##           7 #STR791##     65-(1)           8 #STR792##           9 #STR793##     65-(2)           0 #STR794##           1 #STR795##     65-(3)           2 #STR796##           3 #STR797##     65-(4)           4 #STR798##           5 #STR799##     65-(5)           6 #STR800##           7 #STR801##     65-(6)           8 #STR802##           9 #STR803##     65-(7)           0 #STR804##           1 #STR805##     65-(8)           2 #STR806##           3 #STR807##     65-(9)           4 #STR808##           5 #STR809##     65-(10)           6 #STR810##           7 #STR811##     65-(11)           8 #STR812##           9 #STR813##     65-(12)           0 #STR814##           1 #STR815##     65-(13)           8 #STR816##           2 #STR817##     65-(14)           9 #STR818##           3 #STR819##     65-(15)           4 #STR820##           5 #STR821##     65-(16)           6 #STR822##           7 #STR823##     65-(17)           8 #STR824##           9 #STR825##     65-(18)           0 #STR826##           1 #STR827##     65-(19)           2 #STR828##           3 #STR829##     65-(20)           4 #STR830##           5 #STR831##     65-(21)           6 #STR832##           7 #STR833##     65-(22)           8 #STR834##           9 #STR835##     65-(23)           0 #STR836##           1 #STR837##     65-(24)           2 #STR838##           3 #STR839##     65-(25)           4 #STR840##           5 #STR841##     65-(26)           6 #STR842##           7 #STR843##     65-(27)           8 #STR844##           9 #STR845##     65-(28)           0 #STR846##           1 #STR847##     65-(29)           2 #STR848##           3 #STR849##     65-(30)           4 #STR850##           5 #STR851##     65-(31)           9 #STR852##           6 #STR853##     65-(32)           7 #STR854##           8 #STR855##     65-(33)           9 #STR856##           0 #STR857##     65-(34)           1 #STR858##           2 #STR859##     65-(35)           3 #STR860##           4 #STR861##     65-(36)           5 #STR862##           6 #STR863##     65-(37)           7 #STR864##           8 #STR865##     66-(1)           9 #STR866##           0 #STR867##     66-(2)           1 #STR868##           2 #STR869##     66-(3)           3 #STR870##           4 #STR871##     66-(4)           5 #STR872##           6 #STR873##     66-(5)           7 #STR874##           8 #STR875##     66-(6)           9 #STR876##           0 #STR877##     66-(7)           1 #STR878##           2 #STR879##     66-(8)           3 #STR880##           4 #STR881##     66-(9)           5 #STR882##           6 #STR883##     66-(10)           7 #STR884##           8 #STR885##     66-(11)           9 #STR886##           0 #STR887##     66-(12)           1 #STR888##           2 #STR889##     66-(13)           3 #STR890##           4 #STR891##     66-(14)           5 #STR892##           6 #STR893##     66-(15)           7 #STR894##           8 #STR895##     66-(16)           9 #STR896##           0 #STR897##     66-(17)           1 #STR898##           2 #STR899##     66-(18)           3 #STR900##           4 #STR901##     66-(19)           5 #STR902##           6 #STR903##     66-(20)           7 #STR904##           8 #STR905##     66-(21)           9 #STR906##           0 #STR907##     66-(22)           1 #STR908##           2 #STR909##     66-(23)           3 #STR910##           4 #STR911##     66-(24)           5 #STR912##           6 #STR913##     66-(25)           7 #STR914##           8 #STR915##     66-(26)           9 #STR916##           0 #STR917##     66-(27)           1 #STR918##           2 #STR919##     66-(28)           3 #STR920##           4 #STR921##     66-(29)           5 #STR922##           6 #STR923##     66-(30)           7 #STR924##           8 #STR925##     66-(31)           9 #STR926##           0 #STR927##     66-(32)           1 #STR928##           2 #STR929##     66-(33)           3 #STR930##           4 #STR931##     66-(34)           5 #STR932##           6 #STR933##     66-(35)           7 #STR934##           8 #STR935##     66-(36)           9 #STR936##           0 #STR937##     66-(37)           1 #STR938##           2 #STR939##     67           3 #STR940##           4 #STR941##     68           5 #STR942##           6 #STR943##     69-(1)           7 #STR944##           8 #STR945##     69-(2)           9 #STR946##           0 #STR947##     69-(3)           1 #STR948##           2 #STR949##     69-(4)           3 #STR950##           4 #STR951##     69-(5)           5 #STR952##           6 #STR953##     69-(6)           7 #STR954##           8 #STR955##     69-(7)           9 #STR956##           0 #STR957##     69-(8)           1 #STR958##           2 #STR959##     69-(9)           3 #STR960##           4 #STR961##     69-(10)           5 #STR962##           6 #STR963##     69-(11)           7 #STR964##           8 #STR965##     69-(12)           9 #STR966##           0 #STR967##     69-(13)           1 #STR968##           2 #STR969##     69-(14)           3 #STR970##           4 #STR971##     69-(15)           5 #STR972##           6 #STR973##     70           7 #STR974##           8 #STR975##     71-(1)           9 #STR976##           0 #STR977##     71-(2)           1 #STR978##           2 #STR979##     71-(3)           3 #STR980##           4 #STR981##     71-(4)           5 #STR982##           6 #STR983##     72           7 #STR984##           8 #STR985##     73-(1)           9 #STR986##           0 #STR987##     73-(2)           1 #STR988##           2 #STR989##     74           3 #STR990##           4 #STR991##     75-(1)           5 #STR992##           6 #STR993##     75-(2)           7 #STR994##           8 #STR995##     76           9 #STR996##           0 #STR997##     77           1 #STR998##           2 #STR999##     78           3 #STR1000##           4 #STR1001##     79-(1)           5 #STR1002##           6 #STR1003##     79-(2)           7 #STR1004##           8 #STR1005##     80-(1)           9 #STR1006##           0 #STR1007##     80-(2)           1 #STR1008##           2 #STR1009##     81           9 #STR1010##           3 #STR1011##     82           4 #STR1012##           5 #STR1013##     83           6 #STR1014##           7 #STR1015##     84           8 #STR1016##           9 #STR1017##     85           0 #STR1018##           1 #STR1019##     86           2 #STR1020##           3 #STR1021##     87           4 #STR1022##           5 #STR1023##     88           6 #STR1024##           Object Compound A           7 #STR1025##           Object Compound B           8 #STR1026##     89           9 #STR1027##           0 #STR1028##     90           0 #STR1029##           2 #STR1030##     91           3 #STR1031##           4 #STR1032##     92           4 #STR1033##           1 #STR1034##     93           5 #STR1035##           6 #STR1036##     94           6 #STR1037##           7 #STR1038##     95           8 #STR1039##           9 #STR1040##     96           9 #STR1041##           0 #STR1042##     97           0 #STR1043##           1 #STR1044##     98           1 #STR1045##           2 #STR1046##     99-(1)           3 #STR1047##           4 #STR1048##     99-(2)           5 #STR1049##           6 #STR1050##     99-(3)           7 #STR1051##           8 #STR1052##     99-(4)           9 #STR1053##           0 #STR1054##     99-(5)           1 #STR1055##           2 #STR1056##     99-(6)           3 #STR1057##           4 #STR1058##     99-(7)           5 #STR1059##           6 #STR1060##     99-(8)           7 #STR1061##           8 #STR1062##     99-(9)           9 #STR1063##           0 #STR1064##     99-(10)           1 #STR1065##           2 #STR1066##     99-(11)           3 #STR1067##           4 #STR1068##     99-(12)           5 #STR1069##           6 #STR1070##     99-(13)           7 #STR1071##           8 #STR1072##     99-(14)           9 #STR1073##           0 #STR1074##    100-(1)           1 #STR1075##           2 #STR1076##    100-(2)           3 #STR1077##           4 #STR1078##    100-(3)           5 #STR1079##           6 #STR1080##    100-(4)           7 #STR1081##           8 #STR1082##    100-(5)           9 #STR1083##           0 #STR1084##    100-(6)           1 #STR1085##           2 #STR1086##    100-(7)           3 #STR1087##           4 #STR1088##    100-(8)           5 #STR1089##           6 #STR1090##    100-(9)           7 #STR1091##           8 #STR1092##    100-(10)           9 #STR1093##           0 #STR1094##    100-(11)           1 #STR1095##           2 #STR1096##    100-(12)           3 #STR1097##           4 #STR1098##    100-(13)           5 #STR1099##           6 #STR1100##    100-(14)           7 #STR1101##           8 #STR1102##    101-(1)           5 #STR1103##           9 #STR1104##    101-(2)           7 #STR1105##           0 #STR1106##    101-(3)           8 #STR1107##           1 #STR1108##    101-(4)           5 #STR1109##           2 #STR1110##    101-(5)           9 #STR1111##           3 #STR1112##    101-(6)           5 #STR1113##           4 #STR1114##    101-(7)           5 #STR1115##           6 #STR1116##    102-(1)           7 #STR1117##           8 #STR1118##    102-(2)           9 #STR1119##           0 #STR1120##    102-(3)           1 #STR1121##           2 #STR1122##    102-(4)           3 #STR1123##           4 #STR1124##    102-(5)           5 #STR1125##           6 #STR1126##    102-(6)           7 #STR1127##           8 #STR1128##    102-(7)           9 #STR1129##           0 #STR1130##    103-(1)           1 #STR1131##           2 #STR1132##    103-(2)           3 #STR1133##           4 #STR1134##    103-(3)           5 #STR1135##           6 #STR1136##    104-(1)           9 #STR1137##           7 #STR1138##    104-(2)           9 #STR1139##           8 #STR1140##    104-(3)           5 #STR1141##           9 #STR1142##    104-(4)           5 #STR1143##           0 #STR1144##    104-(5)           5 #STR1145##           1 #STR1146##    105-(1)           2 #STR1147##           3 #STR1148##    105-(2)           8 #STR1149##           4 #STR1150##    105-(3)           9 #STR1151##           5 #STR1152##    105-(4)           0 #STR1153##           6 #STR1154##    105-(5)           1 #STR1155##           7 #STR1156##    106-(1)           8 #STR1157##           9 #STR1158##    106-(2)           0 #STR1159##           1 #STR1160##    106-(3)           2 #STR1161##           3 #STR1162##    106-(4)           4 #STR1163##           5 #STR1164##    106-(5)           6 #STR1165##           7 #STR1166##    106-(6)           8 #STR1167##           9 #STR1168##    106-(7)           0 #STR1169##           1 #STR1170##    106-(8)           2 #STR1171##           3 #STR1172##    106-(9)           4 #STR1173##           5 #STR1174##    106-(10)           6 #STR1175##           7 #STR1176##    107-(1)           8 #STR1177##           9 #STR1178##    107-(2)           0 #STR1179##           1 #STR1180##    107-(3)           2 #STR1181##           3 #STR1182##    107-(4)           4 #STR1183##           5 #STR1184##    107-(5)           6 #STR1185##           7 #STR1186##    107-(6)           8 #STR1187##           9 #STR1188##    107-(7)           0 #STR1189##           1 #STR1190##    107-(8)           2 #STR1191##           3 #STR1192##    107-(9)           4 #STR1193##           5 #STR1194##    107-(10)           6 #STR1195##           7 #STR1196##    108           8 #STR1197##           9 #STR1198##    109           0 #STR1199##           1 #STR1200##    110           0 #STR1201##           2 #STR1202##    111           3 #STR1203##           4 #STR1204##    112-(1)           5 #STR1205##           6 #STR1206##    112-(2)           7 #STR1207##           8 #STR1208##    112-(3)           9 #STR1209##           0 #STR1210##    112-(4)           1 #STR1211##           2 #STR1212##    113-(1)           3 #STR1213##           4 #STR1214##    113-(2)           5 #STR1215##           6 #STR1216##    113-(3)           7 #STR1217##           8 #STR1218##    113-(4)           9 #STR1219##           0 #STR1220##    114-(1)           1 #STR1221##           2 #STR1222##    114-(12)           3 #STR1223##           4 #STR1224##    __________________________________________________________________________

    __________________________________________________________________________    Example No.          Formula    __________________________________________________________________________          1 #STR1225##          2 #STR1226##    2-(1)          1 #STR1227##          3 #STR1228##    2-(2)          4 #STR1229##          5 #STR1230##    2-(3)          4 #STR1231##          6 #STR1232##    2-(4)          4 #STR1233##          7 #STR1234##    2-(5)          4 #STR1235##          8 #STR1236##    2-(6)          4 #STR1237##          9 #STR1238##    2-(7)          0 #STR1239##          1 #STR1240##    2-(8)          2 #STR1241##          3 #STR1242##    2-(9)          4 #STR1243##          5 #STR1244##    2-(10)          6 #STR1245##          7 #STR1246##    2-(11)          8 #STR1247##          9 #STR1248##    2-(12)          0 #STR1249##          1 #STR1250##    2-(13)          2 #STR1251##          3 #STR1252##    3          4 #STR1253##          5 #STR1254##    4-(1)          4 #STR1255##          6 #STR1256##    4-(2)          4 #STR1257##          7 #STR1258##    4-(3)          4 #STR1259##          8 #STR1260##    4-(4)          4 #STR1261##          9 #STR1262##    4-(5)          4 #STR1263##          0 #STR1264##    4-(6)          4 #STR1265##          1 #STR1266##    4-(7)          4 #STR1267##          2 #STR1268##    4-(8)          4 #STR1269##          3 #STR1270##    4-(9)          4 #STR1271##          4 #STR1272##    4-(10)          4 #STR1273##          5 #STR1274##    4-(11)          4 #STR1275##          6 #STR1276##    4-(12)          4 #STR1277##          7 #STR1278##    4-(13)          4 #STR1279##          8 #STR1280##    4-(14)          4 #STR1281##          9 #STR1282##    4-(15)          4 #STR1283##          0 #STR1284##    4-(16)          4 #STR1285##          1 #STR1286##    4-(17)          4 #STR1287##          2 #STR1288##    4-(18)          4 #STR1289##          3 #STR1290##    4-(19)          4 #STR1291##          4 #STR1292##    4-(20)          4 #STR1293##          5 #STR1294##    4-(21)          4 #STR1295##          6 #STR1296##    4-(22)          4 #STR1297##          7 #STR1298##    4-(23)          4 #STR1299##          8 #STR1300##    4-(24)          4 #STR1301##          9 #STR1302##    4-(25)          4 #STR1303##          0 #STR1304##    4-(26)          5 #STR1305##          1 #STR1306##    4-(27)          4 #STR1307##          2 #STR1308##    4-(28)          4 #STR1309##          3 #STR1310##    4-(29)          4 #STR1311##          4 #STR1312##    4-(30)          4 #STR1313##          5 #STR1314##    4-(31)          6 #STR1315##          7 #STR1316##    5          7 #STR1317##          8 #STR1318##    6          9 #STR1319##          0 #STR1320##    7          1 #STR1321##          2 #STR1322##    8          3 #STR1323##          Compound A          4 #STR1324##          5 #STR1325##    9-(1)          6 #STR1326##          7 #STR1327##    9-(2)          7 #STR1328##          8 #STR1329##    9-(3)          9 #STR1330##          0 #STR1331##    9-(4)          8 #STR1332##          9 #STR1333##    9-(5)          0 #STR1334##          1 #STR1335##    9-(6)          2 #STR1336##          3 #STR1337##    9-(7)          4 #STR1338##          5 #STR1339##    9-(8)          6 #STR1340##          7 #STR1341##    9-(9)          8 #STR1342##          9 #STR1343##    9-(10)          0 #STR1344##          1 #STR1345##    9-(11)          2 #STR1346##          3 #STR1347##    9-(12)          4 #STR1348##          5 #STR1349##    9-(13)          6 #STR1350##          7 #STR1351##    9-(14)          6 #STR1352##          8 #STR1353##    9-(15)          9 #STR1354##          0 #STR1355##    9-(16)          1 #STR1356##          2 #STR1357##    9-(17)          6 #STR1358##          3 #STR1359##    9-(18)          4 #STR1360##          5 #STR1361##    9-(19)          6 #STR1362##          7 #STR1363##    10-(1)          8 #STR1364##          9 #STR1365##    10-(2)          0 #STR1366##          1 #STR1367##    10-(3)          2 #STR1368##          3 #STR1369##    10-(4)          2 #STR1370##          4 #STR1371##    10-(5)          5 #STR1372##          6 #STR1373##    10-(6)          5 #STR1374##          7 #STR1375##    10-(7)          8 #STR1376##          9 #STR1377##    10-(8)          8 #STR1378##          0 #STR1379##    10-(9)          1 #STR1380##          2 #STR1381##    10-(10)          1 #STR1382##          3 #STR1383##    10-(11)          4 #STR1384##          5 #STR1385##    10-(12)          4 #STR1386##          6 #STR1387##    10-(13)          7 #STR1388##          8 #STR1389##    10-(14)          7 #STR1390##          9 #STR1391##    10-(15)          0 #STR1392##          1 #STR1393##    10-(16)          0 #STR1394##          2 #STR1395##    10-(17)          3 #STR1396##          4 #STR1397##    10-(18)          5 #STR1398##          6 #STR1399##    10-(19)          5 #STR1400##          7 #STR1401##    10-(20)          8 #STR1402##          9 #STR1403##    10-(21)          8 #STR1404##          0 #STR1405##    10-(22)          8 #STR1406##          1 #STR1407##    10-(23)          2 #STR1408##          3 #STR1409##    10-(24)          2 #STR1410##          4 #STR1411##    10-(25)          1 #STR1412##          2 #STR1413##    10-(26)          3 #STR1414##          4 #STR1415##    10-(27)          5 #STR1416##          6 #STR1417##    10-(28)          5 #STR1418##          7 #STR1419##    10-(29)          1 #STR1420##          8 #STR1421##    10-(30)          9 #STR1422##          0 #STR1423##    10-(31)          9 #STR1424##          1 #STR1425##    10-(32)          9 #STR1426##          2 #STR1427##    10-(33)          3 #STR1428##          4 #STR1429##    10-(34)          5 #STR1430##          6 #STR1431##    10-(35)          5 #STR1432##          7 #STR1433##    10-(36)          8 #STR1434##          9 #STR1435##    10-(37)          8 #STR1436##          0 #STR1437##    10-(38)          8 #STR1438##          1 #STR1439##    10-(39)          2 #STR1440##          3 #STR1441##    10-(40)          2 #STR1442##          4 #STR1443##    10-(41)          1 #STR1444##          5 #STR1445##    10-(42)          6 #STR1446##          7 #STR1447##    10-(43)          6 #STR1448##          8 #STR1449##    10-(44)          6 #STR1450##          9 #STR1451##    10-(45)          0 #STR1452##          1 #STR1453##    10-(46)          3 #STR1454##          2 #STR1455##    10-(47)          3 #STR1456##          4 #STR1457##    10-(48)          3 #STR1458##          5 #STR1459##    10-(49)          6 #STR1460##          7 #STR1461##    10-(50)          8 #STR1462##          9 #STR1463##    10-(51)          0 #STR1464##          1 #STR1465##    10-(52)          0 #STR1466##          2 #STR1467##    10-(53)          3 #STR1468##          4 #STR1469##    10-(54)          5 #STR1470##          6 #STR1471##    10-(55)          5 #STR1472##          6 #STR1473##    10-(56)          7 #STR1474##          8 #STR1475##    10-(57)          9 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Preparation 1

Starting Compound (2.00 g), 1-methylpiperazine (414 mg), and1-hydroxybenzotriazole (559 mg) were dissolved in methylene chloride (50ml). The mixture was ice-cooled and1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (793 mg) wasadded thereto. The mixture was stirred at this temperature for 1 hourand at room temperature for 4 hours. The mixture was concentrated undervacuum and the residue was diluted in water and extracted withchloroform. The organic layer was washed with saturated sodiumhydrogencarbonate solution and brine. After evaporation, the crudematerial obtained was purified on a column of silica gel eluting withchloroform-methanol (60:1) to give Object Compound (2.34 g) as anamorphous solid.

MASS (FAB) (m/z): 566 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.29 (3H,s), 2.32-2.47 (4H, m), 2.52 (3×2/3H, s), 2.55-2.61 (1H, m), 2.77(3×1/3H, s), 2.95-3.10 (2H, m), 3.16-3.27 (1H, m), 3.42-3.50 (2H, m),3.57-3.63 (2H, m), 4.07-4.32 (2×2/3H, m), 4.47-4.58 (1H, m), 4.62(2×1/3H, d, J=15 Hz), 5.09-5.17 (1H, m), 6.00-6.07 (1H, m), 6.83-6.90(1H, m), 7.00-7.05 (1H, m), 7.18-7.30 (8H, m), 7.40 (1×1/3H, d, J=8 Hz),7.43 (1×2/3H, d, J=8 Hz)

Preparation 2

The following object compound was obtained according to a similar mannerto that of Preparation 1.

Mass (FAB) (m/z): 553 (M+H)⁺ ; NMR (CDCl₃, δ): 1.43 (9H, s), 2.50-2.62(1H, m), 2.54 (3×2/3H, s), 2.79 (3×1/3H, s), 2.96-3.10 (2H, m),3.15-3.25 (1H, m), 3.42-3.48 (2H, m), 3.58-3.62 (2H, m), 3.65-3.72 (4H,m), 4.04-4.33 (2×2/3H, m), 4.50-4.58 (1H, m), 4.62 (2×1/3H, d, J=15 Hz),5.08-5.17 (1H, m), 6.00 (1H, d, J=8 Hz), 6.87-7.05 (2H, m), 7.18-7.27(8H, m), 7.40 (1×1/3H, d, J=8 Hz), 7.46 (1×2/3H, d, J=8 Hz)

Preparation 3

Starting Compound (2.34 g) was dissolved in methylene chloride (20 ml)and the solution was ice-cooled. To this solution was addedtrifluoroacetic acid (10 ml). The mixture was stirred at thistemperature for 10 minutes and at room temperature for 1 hour and wasconcentrated under reduced pressure. The residue was made alkaline withsaturated sodium hydrogencarbonate solution and extracted withchloroform. The organic layer was washed with brine and evaporated underreduced pressure to give Object Compound (1.46 g) as an amorphous solid.

Mass (FAB) (m/z): 466 (M+H)⁺ ; NMR (CDCl₃, δ): 2.23-2.50 (5H, m), 2.29(3H, s), 2.63 (3×2/3H, s), 2.70-2.85 (1H, m), 2.87 (3×1/3H, s),2.93-3.13 (2H, m), 3.39 (1H, t, J=5 Hz), 3.46 (1H, t, J=5 Hz), 3.52-3.73(3H, m), 4.31-4.38 (2×2/3H, m), 4.67 (2×1/3H, d, J=15 Hz), 5.11-5.20(1H, m), 6.94-7.13 (2H, m), 7.18-7.31 (8H, m), 8.04 (1×1/3H, d, J=8 Hz),8.15 (1×2/3H, d, J=8 Hz)

Preparation 4

A mixture of Starting Compound (0.15 g) and trifluoroacetic acid (0.5ml) was stirred at room temperature for 1 hour. Trifluoroacetic acid wasremoved under reduced pressure. The residue was dissolved in 10%hydrochloric acid-methanol (0.2 ml). Evaporation of solvent gave ObjectCompound (0.15 g) as powder.

NMR (CD₃ OD, δ): 2.90 (3×2/3H, s), 2.97 (3H, s), 3.05 (3×1/3H, s),3.03-3.16 (4H, m), 3.42-3.62 (8H, m), 4.27 (1H, m), 4.50-4.68 (2H, m),5.46 (1H, t, J=7 Hz), 7.18-7.36 (5H, m), 7.83-8.04 (2H, m), 8.48 (1H,m), 8.76 (1H, d, J=6 Hz)

Preparation 5

The following object compounds were obtained according to a similarmanner to that of Preparation 3 or 4.

(1) MASS (FAB) (m/z): 453 (M+H)⁺ ; NMR (CDCl₃, δ): 2.43-2.53 (1H, m),2.67 (3×2/3H, s), 2.71-2.83 (1H, m), 2.87 (3×1/3H, s), 2.93-3.13 (2H,m), 3.37-3.45 (2H, m), 3.54-3.73 (7H, m), 4.29-4.43 (2×2/3H, m), 4.68(2×1/3H, d, J=15 Hz), 5.12-5.21 (1H, m), 6.95-7.15 (2H, m), 7.20-7.31(8H, m), 8.07 (1×1/3H, d, J=8 Hz), 8.15 (1×2/3H, d, J=8 Hz)

(2) MASS (FAB) (m/z): 474 (M+H)⁺ ; NMR (CDCl₃, δ): 2.42-2.63 (1H, m),2.67 (3×2/3H, s), 2.81-2.91 (1H, m), 2.86 (3×1/3H, s), 2.95-3.15 (2H,m), 3.60-3.65 (1×1/3H, m), 3.70-3.74 (1×2/3H, m), 4.22-4.41 (2×2/3H, m),4.67 (2×1/3H, d, J=15 Hz), 5.08-5.18 (3H, m), 6.96-7.29 (12H, m),7.30-7.41 (3H, m), 8.00 (1×1/3H, d, J=8 Hz), 8.08 (1×2/3H, d, J=8 Hz)

(3) NMR (CDCl₃, δ): 2.36 (1H, dd, J=7, 15 Hz), 2.72-2.78 (2H, m), 2.95(1H, dd, J=7, 15 Hz), 3.22 (3H, s), 3.37 (2H, m), 3.50-3.70 (7H, m),4.77 (1H, q, J=7 Hz), 6.87 (2H, m), 6.93 (2H, m), 7.20-7.22 (4H, m),7.31-7.34 (4H, m), 7.94 (1H, d, J=7 Hz)

(4) NMR (CD₃ OD, δ): 2.91-3.00 (2H, m), 2.92 (3×1/3H, s), 3.03 (3×2/3H,s), 3.41-3.68 (10H, m), 4.24 (1H, m), 4.50-4.60 (2H, m), 5.42 (1H, m),7.18-7.21 (2H, m), 7.29-7.36 (3H, m), 7.76-7.80 (2H, m), 8.28 (1H, m),8.67 (1H, m)

(5) NMR (CD₃ OD, δ): 2.87 (6×2/3H, s), 2.97 (3H, s), 2.98 (6×1/3H, s),3.05-3.14 (4H, m), 3.22 (1H, m), 3.35 (1H, m), 3.49-3.74 (9H, m), 4.02(1H, m), 4.27 (1H, m), 4.94 (1H, t, J=7 Hz), 7.27-7.36 (5H, m)

(6) NMR (CDCl₃, δ): 1.77 (1H, m), 2.18 (3H, s), 2.13-2.33 (3H, m), 2.49(1H, dd, J=7, 15 Hz), 2.78 (1H, dd, J=3, 15 Hz), 3.00 (2H, d, J=7 Hz),3.02 (1H, m), 3.33 (1H, m), 3.43 (2H, m), 3.52-3.72 (9H, m), 5.12 (1H,q, J=7 Hz), 7.19-7.31 (5H, m), 8.14 (1H, d, J=7 Hz)

(7) NMR (DMSO-d₆, δ): 1.11 (3H, t, J=7 Hz), 2.81-3.10 (4H, m), 4.03 (2H,q, J=7 Hz), 4.13 (1H, m), 4.52 (1H, q, J=7 Hz), 5.14 (1H, d, J=15 Hz),5.19 (1H, d, J=15 Hz), 7.24-7.32 (5H, m), 7.37-7.41 (4H, m), 8.28 (3H,m), 8.94 (1H, d, J=8 Hz)

Preparation 6

To a stirred mixture of Starting Compound (2.00 g), 1-methylpiperazine(0.62 g) and 1-hydroxybenzotriazole (0.84 g) in methylene chloride (30ml) was added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimidehydrochloride (1.20 g) in some portions at 0° C. and the mixture wasstirred at room temperature for 4 hours. The reaction mixture was washedwith 5% aqueous sodium bicarbonate twice and dried. Evaporation ofsolvent gave a residue which was purified by silica gel columnchromatography. Elution with chloroform˜3% methanol-chloroform affordedObject Compound (2.50 g) as powder.

MASS (FAB) (m/z): 406 (M⁺ +1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.30 (3H,s), 2.35 (4H, m), 2.77 (1H, dd, J=4, 16 Hz), 3.15 (1H, dd, J=4, 16 Hz),3.42 (2H, t, J=5 Hz), 3.57 (2H, m), 4.60 (1H, m), 5.13 (1H, d, J=15 Hz),5.22 (1H, d, J=15 Hz), 5.82 (1H, d, J=7 Hz), 7.33 (5H, m)

Preparation 7

The following object compound was obtained according to a similar mannerto that of Preparation 6.

NMR (CDCl₃, δ): 1.44 (9H, s), 2.78 (1H, dd, J=4, 16 Hz), 3.11 (1H, dd,J=4, 16 Hz), 3.43 (2H, t, J=7 Hz), 3.58 (2H, m), 3.67 (4H, m), 3.76 (3H,s), 4.58 (1H, td, J=4, 7 Hz), 5.75 (1H, d, J=7 Hz)

Preparation 8

A mixture of Starting Compound (0.7 g) and trifluoroacetic acid (1.5 ml)was stirred at room temperature for 1 hour. Evaporation oftrifluoroacetic acid gave a residue which was made alkaline with 1Naqueous sodium hydroxide and extracted with chloroform. The extract waswashed with water and dried. Evaporation of solvent gave Object Compound(0.39 g).

NMR (CDCl₃, δ): 1.85 (1H, m), 2.22 (3H, s), 2.20-2.37 (3H, m), 2.80 (1H,dd, J=7, 12 Hz), 2.92 (1H, dd, J=7, 12 Hz), 3.09 (1H, m), 3.34 (1H, m),3.60 (2H, m), 3.94 (1H, t, J=7 Hz), 7.17-7.32 (5H, m)

Preparation 9

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4 or 8.

(1) NMR (CD₃ OD, δ): 2.95 (3×1/3H, s), 2.97 (3×2/3H, s), 3.45-3.59 (2H,m), 4.50 (1H, d, J=15 Hz), 4.66 (1H, d, J=15 Hz), 5.02 (1H, m),7.20-7.37 (5H, m), 7.75-7.82 (2H, m), 8.28 (1H, m), 8.71 (1H, d, J=4 Hz)

(2) NMR (CDCl₃, δ): 2.18 (6×2/5H, s), 2.26 (6×3/5H, s), 2.12-2.33 (1H,m), 2.40 (1H, t, J=7 Hz), 2.79 (3×3/5H, s), 2.77 (1H, m), 2.92 (3×2/5H,s), 2.94 (1H, m), 3.02 (1×2/5H, m), 3.23 (1×2/5H, m), 3.46 (2×3/5H, m),3.87 (1×2/5H, t, J=7 Hz), 3.91 (1×3/5H, t, J=7 Hz), 7.19-7.32 (5H, m)

Preparation 10

A solution of Starting Compound (2.6 g) in methanol (50 ml) washydrogenated over 10% palladium on carbon (0.7 g) at 4 kg/cm⁻² for 6hours. The catalyst was filtered off and washed with methanol. Thecombined filtrate and washings were evaporated to give Object Compound(2.00 g) as powder.

MASS (FAB) (m/z): 316 (M⁺ +1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.78 (3H,s), 2.82 (1H, m), 3.02-3.20 (5H, m), 3.83 (4H, m), 4.43 (1H, m), 5.89(1H, d, J=7 Hz)

Preparation 11

To a stirred solution of Starting Compound (0.5 g) and triethylamine(0.24 ml) in N,N-dimethylformamide (6 ml) was added dropwisetrimethylacetyl chloride (0.21 ml) at -10° C. and the mixture wasstirred at 0° C. for 5 minutes. To this solution was added dropwise asolution of N-methylaniline (0.18 g) in N,N-dimethylformamide (1 ml) at-10° C. and the mixture was stirred at room temperature overnight. Thereaction mixture was diluted with water and extracted with chloroform.The extract was washed with 1N aqueous hydrochloric acid and 5% aqueoussodium bicarbonate, and dried. Evaporation of solvent gave a residuewhich was chromatographed on silica gel. Elution with chloroform gaveObject Compound (0.49 g).

MASS (FAB) (m/z): 389 (M⁺ +1); NMR (CDCl₃, δ): 2.72 (1H, dd, J=7, 12Hz), 2.90 (1H, dd, J=7, 12 Hz), 3.20 (3H, s), 4.57 (1H, q, J=7 Hz), 5.00(1H, d, J=15 Hz), 5.06 (1H, d, J=15 Hz), 5.43 (1H, d, J=7 Hz), 6.83-6.90(4H, m), 7.21 (3H, m), 7.32-7.33 (8H, m)

Preparation 12

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6 or 11.

(1) MASS (FAB) (m/z): 370 (M⁺ +1); NMR (CDCl₃, δ): 1.39 (9H, s), 2.87(3×1/4H, s), 2.95 (3×3/4H, s), 3.06 (1H, dd, J=7, 14 Hz), 3.22 (1H, dd,J=7, 14 Hz), 4.40 (1H, d, J=15 Hz), 4.71 (1H, d, J=15 Hz), 5.14 (1H, m),5.48 (1H, d, J=7 Hz), 7.14-7.16 (4H, m), 7.23-7.32 (3H, m), 7.55 (1H,m), 8.51 (1H, d, J=4 Hz)

(2) MASS (FAB) (m/z): 350 (M⁺ +1); NMR (CDCl₃, δ): 1.40 (9H, s), 2.16(6×1/3H, s), 2.23 (6×2/3H, s), 2.10-2.37 (2H, m), 2.68 (3×2/3H, s), 2.88(3×1/3H, s), 2.95 (2H, d, J=7 Hz), 2.97-3.12 (2×1/3H, m), 3.27-3.50(2×2/3H, m), 4.80 (1H, m), 5.32 (1×1/3H, d, J=7 Hz), 5.38 (1×2/3H, d,J=7 Hz), 7.19-7.28 (5H, m)

(3) MASS (FAB) (m/z): 348 (M⁺ +1); NMR (CDCl₃, δ): 1.42 (9H, s), 1.75(1H, m), 2.18 (3H, s), 2.14-2.32 (3H, m), 2.89-3.02 (3H, m), 3.26-3.34(1H, m), 3.52-3.57 (2H, m), 4.82 (1H, m), 5.42 (1H, d, J=7 Hz),7.17-7.30 (5H, m)

(4) MASS (FAB) (m/z): 406 (M⁺ +1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.47(1H, dd, J=7, 16 Hz), 2.80 (2H, t, J=7 Hz), 3.18 (1H, dd, J=4, 16 Hz),3.35-3.70 (10H, m), 4.51 (1H, m), 6.03 (1H, d, J=7 Hz), 6.82 (1H, m),7.18-7.32 (5H, m)

Preparation 13

To a stirred solution of Starting Compound (3.8 g) in methanol (30 ml)was added dropwise 1N aqueous sodium hydroxide (12 ml) at 0° C. and themixture was stirred at room temperature for 4 hours. The reactionmixture was diluted with water and extracted with ether. The aqueoussolution was acidified with 10% aqueous citric acid and extracted withchloroform 4 times and dried. Evaporation of solvent gave ObjectCompound (3.55 g) as powder.

NMR (CDCl₃, δ): 1.44 (9H, s), 2.70 (1H, dd, J=7, 16 Hz), 3.20 (1H, dd,J=4, 16 Hz), 3.48 (2H, m), 3.64-3.75 (6H, m), 4.55 (1H, dt, J=4, 7 Hz),5.82 (1H, d, J=7 Hz)

Preparation 14

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6 or 11.

(1) MASS (FAB) (m/z): 567 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.29(3H, s), 2.38 (4H, m), 2.55 (1H, dd, J=5, 15 Hz), 2.82 (3×1/3H, s), 2.90(3×2/3H, s), 3.07-3.32 (3H, m), 3.45 (2H, m), 3.58 (2H, m), 4.25 (1H,m), 4.46-4.65 (2H, m), 4.79 (1H, dd, J=4, 15 Hz), 5.40 (1H, m), 6.03(1H, m), 7.06-7.32 (6H, m), 7.51-7.62 (2H, m), 8.47 (1H, d, J=5 Hz)

(2) MASS (FAB) (m/z): 554 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.82(3×1/3H, s), 2.91 (3×2/3H, s), 3.07-3.33 (4H, m), 3.42 (2H, m),3.56-3.67 (6H, m), 4.17 (1H, d, J=15 Hz), 4.28 (1H, d, J=15 Hz), 4.51(1H, m), 4.79 (1H, m), 5.40 (1H, m), 6.02 (1H, m), 7.07-7.31 (6H, m),7.51-7.62 (2H, m), 8.48 (1H, d, J=5 Hz)

(3) MASS (FAB) (m/z): 539 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.53(1H, dd, J=5, 15 Hz), 2.72 (1H, dd, J=7, 13 Hz), 2.93 (1H, dd, J=7, 13Hz), 3.16 (3H, s), 3.16 (1H, m), 3.43 (2H, m), 3.57 (2H, m), 3.66 (4H,m), 4.52 (1H, m), 4.74 (1H, m), 5.97 (1H, d, J=7 Hz), 6.72 (2H, m), 6.97(2H, m), 7.21-7.33 (7H, m)

(4) MASS (FAB) (m/z): 534 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.13(6×2/5H, s), 2.22 (6×3/5H, s), 2.28 (1H, m), 2.52 (1×2/5H, m), 2.58(1×3/5H, m), 2.62 (3×3/5H, s), 2.85 (3×2/5H, s), 2.94-3.05 (3H, m),3.16-3.29 (2H, m), 3.41-3.51 (3H, m), 3.59 (2H, m), 3.67 (4H, m), 4.51(1H, m), 5.02 (1H, m), 5.98 (1H, d, J=7 Hz), 7.22-7.27 (5H, m), 7.35(1×2/5H, d, J=7 Hz), 7.41 (1×3/5H, d, J=7 Hz)

(5) MASS (FAB) (m/z): 532 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 1.70(1H, m), 2.17 (3H, s), 2.11-2.19 (2H, m), 2.28 (1H, m), 2.55 (1H, dd,J=5, 16 Hz), 2.86-3.06 (3H, m), 3.18-3.28 (2H, m), 3.43-3.72 (10H, m),4.53 (1H, m), 5.06 (1H, m), 6.00 (1H, d, J=7 Hz), 7.20-7.30 (5H, m),7.42 (1H, d, J=7 Hz)

(6) NMR (CDCl₃, δ): 1.20 (3H, t, J=7 Hz), 1.42 (9H, s), 2.70 (1H, dd,J=7, 16 Hz), 3.08 (2H, d, J=7 Hz), 3.07 (1H, dd, J=4, 16 Hz), 4.13 (2H,q, J=7 Hz), 4.52 (1H, m), 4.77 (1H, q, J=7 Hz), 5.10 (1H, d, J=15 Hz),5.15 (1H, d, J=15 Hz), 5.62 (1H, d, J=7 Hz), 6.93 (1H, d, J=7 Hz), 7.14(2H, d, J=8 Hz), 7.23-7.35 (8H, m)

Preparation 15

The following object compound was obtained according to a similar mannerto that of Preparation 1, 6 or 11.

MASS (FAB) (m/z): 360 (M⁺ +1); NMR (CDCl₃, δ): 2.88 (1H, dd, J=4, 16Hz), 3.25 (1H, dd, J=4, 16 Hz), 3.42-3.45 (2H, m), 3.58-3.62 (2H, m),3.65-3.69 (4H, m), 3.77 (3H, s), 5.13 (1H, dt, J=4, 7 Hz), 6.99 (1H, s),7.14 (1H, t, J=8 Hz), 7.29 (1H, t, J=8 Hz), 7.42 (1H, d, J=8 Hz), 7.55(1H, d, J=8 Hz), 7.66 (1H, d, J=8 Hz), 9.25 (1H, br s)

Preparation 16

The following object compound was obtained according to a similar mannerto that of Preparation 13.

MASS (FAB) (m/z): 346 (M⁺ +1); NMR (CDCl₃, δ): 2.83 (1H, dd, J=7, 16Hz), 3.33 (1H, m), 3.44 (2H, m), 3.65 (6H, m), 5.02 (1H, t, J=7 Hz),7.04 (1H, s), 7.12 (1H, t, J=8 Hz), 7.27 (1H, t, J=8 Hz), 7.42 (1H, d,J=8 Hz), 7.64 (1H, d, J=8 Hz), 7.69 (1H, br s), 9.57 (1H, br s)

Preparation 17

The following object compound was obtained according to a similar mannerto that of Preparation 10.

NMR (CDCl₃, δ): 2.59 (1H, dd, J=7, 14 Hz), 2.94 (1H, dd, J=7, 14 Hz),3.22 (3H, s), 3.55 (1H, t, J=7 Hz), 6.82 (2H, m), 6.90 (2H, m),7.20-7.22 (4H, m), 7.32-7.35 (4H, m)

Preparation 18

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4 or 8.

(1) NMR (CD₃ OD, δ): 2.77-2.92 (4H, m), 3.37-3.47 (3H, m 3.52-3.67 (7H,m), 4.13 (1H, t, J=7 Hz), 7.17-7.32 (5H, m)

(2) NMR (CD₃ OD, δ): 3.03 (1H, dd, J=4, 16 Hz), 3.18 (1H, dd, J=7, 16Hz), 3.50 (2H, t, J=7 Hz), 3.56(2H, t, J=7 Hz), 3.63-3.70 (4H, m), 3.82(3H, s), 4.32 (1H, dd, J=4, 7 Hz)

Preparation 19

The following object compound was obtained according to a similar mannerto that of Preparation 1, 6 or 11.

MASS (FAB) (m/z): 449 (M⁺ +1); NMR (CDCl₃, δ): 2.51 (1H, dd, J=7, 16Hz), 2.79 (2H, t, J=7 Hz), 3.31 (1H, dd, J=4, 16 Hz), 3.36-3.60 (6H, m),3.62-3.68 (4H, m), 5.03 (1H, dd, J=4, 7 Hz), 6.95 (1H, d, J=2 Hz), 7.03(1H, t, J=7 Hz), 7.09-7.22 (5H, m), 7.32 (1H, t, J=8 Hz), 7.45 (1H, d,J=8 Hz), 7.67 (1H, d, J=8 Hz), 8.11 (1H, d, J=8 Hz), 9.43 (1H, br s)

Preparation 20

The following object compound was obtained according to a similar mannerto that of Preparation 1, 6 or 11.

MASS (FAB) (m/z): 438 (M⁺ +1);

NMR (CDCl₃, δ): 2.47-2.65 (2H, m), 2.62 (3×2/3H, s), 2.67 (3×1/3H, s),3.05 (4H, m), 3.48 (2H, m), 3.62-3.70 (6H, m), 4.17 (1×1/3H, d, J=15Hz), 4.38 (1×2/3H, d, J=15 Hz), 4.45 (1×1/3H, d, J=15 Hz), 4.62 (1×2/3H,d, J=15 Hz), 5.17 (1H, m), 7.11-7.31 (11H, m)

Preparation 21

A mixture of Starting Compound (6.22 g), 1H-1,2,4-triazole (4.15 g), andpotassium carbonate (8.29 g) in N,N-dimethylformamide (50 ml) was heatedto 120° C. for 1.5 hours. The mixture was concentrated, thereto addedwater (150 ml), and extracted three times with ethyl acetate. Theorganic layer was washed with water, brine, and dried over magnesiumsulfate. The solvent was evaporated, and the residue was passed througha short column of silica gel eluting with a mixture of methylenechloride and ethyl acetate. Evaporation of the solvent gave ObjectCompound as white crystals.

MASS (m/z): 174 (M+H)⁺ ; NMR (CDCl₃, δ): 7.92 (2H, d, J=9 Hz), 8.06 (2H,d, J=9 Hz), 8.17 (1H, s), 8.69 (1H, s), 10.07 (1H, s)

Preparation 22

Starting Compound (5.19 g) was dissolved in 30% methylamine in methanol(30 ml), and heated to 60° C. for 1 hour. Evaporation of the solventgave a solid, and the solid was suspended in ethanol (150 ml), thencooled with ice. To this suspension was added sodium borohydride (1.13g) in some portions and the mixture was stirred at room temperature for1 hour. The mixture was concentrated, thereto added some water, andextracted five times with dichloromethane. The organic layer was washedwith brine, and dried over potassium carbonate. Evaporation of thesolvent, followed by distillation (bp 136-137° C./0.45 mmHg) affordedObject Compound as colorless prisms (4.00 g).

mp: 55-56° C.; MASS (m/z): 189 (M+H)⁺ ; NMR (CDCl₃, δ): 2.46 (3H, s),3.80 (2H, s), 7.46 (2H, d, J=8 Hz), 7.62 (2H, d, J=8 Hz), 8.10 (1H, s),8.52 (1H, s)

Preparation 23

Starting Compound (729 mg) was dissolved in 30% methylamine in methanol(3 ml), and heated to 60° C. for 1.5 hours. Evaporation of the solventgave an oil, and the residue was redissolved in ethanol (5 ml), thencooled with ice. To this solution was added sodium borohydride (204 mg)in some portions and the mixture was stirred at room temperature for 1hour. After the mixture was concentrated, added aqueous sodiumhydroxide, and extracted three times with chloroform. The organic layerwas dried over magnesium sulfate and evaporated. The product waspurified by column chromatography (silica gel) eluting with a mixture ofchloroform and methanol to give Object Compound as a pale-yellow oil(316 mg).

MASS (m/z): 153 (M+H)⁺ ; NMR (CDCl₃, δ): 2.45 (3H, s), 3.69 (2H, s),3.92 (3H, s), 6.72 (1H, d, J=9 Hz), 7.58 (1H, dd, J=9, 2 Hz), 8.08 (1H,d, J=2 Hz)

Preparation 24

Object Compound was obtained according to a similar manner to that ofPreparation 23.

MASS (m/z): 157 (M+H)⁺ ; NMR (CDCl₃, δ): 2.46 (3H, s), 3.77 (2H, s),7.71 (1H, s), 8.42 (1H, s), 8.48 (1H, s)

Preparation 25

A mixture of Starting Compound (3.0 g) and 30% methylamine-methanol (30ml) was stirred at 60° C. for 2 hours. Evaporation of methanol gave aresidue, which was redissolved in methanol (30 ml). To this mixture wasadded sodium borohydride (0.5 g) in some portions at 0° C. The mixturewas stirred at room temperature for 30 minutes. The reaction mixture wasmade acidic with 1N hydrochloric acid and extracted with ether. Theaqueous solution was made alkaline with 1N aqueous sodium hydroxide andextracted with chloroform. The extract was washed with water and dried.Evaporation of solvent gave Object Compound (2.4 g).

MASS (m/z): 190 (M⁺ +1); NMR (CDCl₃, δ): 2.45 (3H, s), 3.81 (2H, s),7.43 (2H, d, J=8 Hz), 7.57 (2H, d, J=8 Hz)

Preparation 26

To an ice-cooled solution of di-tert-butyl dicarbonate (4.50 g) indichloromethane (10 ml) was added Starting Compound (2.51 g), and themixture was stirred at room temperature for 1 hour. The mixture wasdiluted with dichloromethane, washed with water, brine, and dried overmagnesium sulfate. Evaporation of the solvent afforded Object Compound(4.51 g) as a pale-yellow crystal.

mp: 55-57° C.; MASS (m/z): 226 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45 (9H, s),4.28 (2H, br d), 4.84 (1H, br s), 6.93-7.05 (2H, m), 7.20-7.30 (2H, m)

Preparation 27

To an ice-cooled suspension of Starting Compound (6.05 g) indichloromethane (40 ml) was added triethylamine (5 ml). Di-tert-butyldicarbonate (6.78 g) in dichloromethane (20 ml) was added theretodropwise, and the mixture was stirred at room temperature for 8 hours.The mixture was washed twice with 10% citric acid, once with aqueoussodium hydrogencarbonate, once with brine, and dried over magnesiumsulfate. Evaporation of the solvent gave Object Compound (7.89 g) as awhite solid.

MASS (m/z): 266 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45 (9H, s), 3.89 (3H, s),4.35 (2H, br s), 4.95 (1H, br s), 7.33 (2H, d, J=8 Hz), 7.98 (2H, d, J=8Hz)

Preparation 28

To an ice-cooled suspension of sodium hydride (600 mg) in anhydroustetrahydrofuran (10 ml) was added dropwise Starting Compound (4.51 g) inanhydrous tetrahydrofuran (10 ml) for 5 minutes. The mixture was heatedto 60° C. for 2 hours. During the heating, the mixture turned into lightyellow. After the mixture was allowed to cool to room temperature,iodomethane (4.56 g) was added thereto dropwise and heated to 30° C. for2 hours. The reaction mixture was allowed to cool to room temperature.Water was added thereto, and the mixture was extracted three times withether. The organic layer was washed with brine and dried over magnesiumsulfate. After the solvent was evaporated, the residue was subjected tocolumn chromatography (silica gel, hexane--ethyl acetate) to give ObjectCompound (3.09 g) as a colorless oil.

MASS (m/z): 240 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.80 (3H, s),4.38 (2H, s), 6.92-7.05 (2H, m), 7.10-7.27 (2H, m)

Preparation 29

To an ice-cooled suspension of sodium hydride (0.86 g) in anhydroustetrahydrofuran (30 ml) was added dropwise Starting Compound (7.89 g) inanhydrous tetrahydrofuran (15 ml) for 10 minutes. The mixture was heatedto 40° C. for 2 hours. During the heating, the mixture turned into lightyellow. After the mixture was allowed to cool to room temperature,iodomethane (5.02 g) was-added dropwise and heated to 40° C. for 2hours. The reaction mixture was allowed to cool to room temperature.Water was added to the mixture, and the mixture was extracted threetimes with ether. The organic layer was washed with brine and dried overmagnesium sulfate. After the solvent was evaporated, the residue wassubjected to column chromatography (silica gel, hexane--ethyl acetate)to give Object Compound (5.21 g) as a colorless oil.

MASS (m/z): 280 (M+H)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, br s), 2.80 (1/2×2H,br s), 2.88 (1/2×2H, br s), 3.90 (3H, s), 4.47 (2H, br s), 7.28 (2H, d,J=8 Hz), 8.00 (2H, d, J=8 Hz)

Preparation 30

10% Hydrogen chloride in methanol (50 ml) was added to Starting Compound(7.56 g) and heated to 60° C. for 3 hours. The mixture was allowed tocool to room temperature. The white precipitate formed was collected byfiltration and washed with ether. The product was recrystallized fromethanol-water (10:1) to give Object Compound (6.15 g).

NMR (D₂ O, δ): 3.95 (3H, s), 4.28 (2H, s), 7.59 (2H, d, J=8 Hz), 8.11(2H, d, J=8 Hz)

Preparation 31

Starting Compound (12.09 g), 37% formaldehyde solution (16.5 ml), andformic acid (9.1 ml) were mixed with ice-cooling and heated to 80° C.for 20 hours. After the mixture was allowed to cool to room temperature,6N hydrochloric acid (20 ml) was added and washed with ether. Theaqueous layer was adjusted to pH 6-7 by adding 28% aqueous ammonia andthen concentrated. Acetone was added to the solution, and the whiteprecipitate formed was filtered, washed with acetone and ether, andevaporated in vacuo to give Object Compound (4.34 g).

mp: >300° C. (dec.); NMR (D₂ O): 2.89 (6H, s), 4.38 (2H, s), 7.57 (2H,d, J=8 Hz), 7.96 (2H, d, J=8 Hz)

Preparation 32

A mixture of Starting Compound (3.59 g), methylamine hydrochloride (1.36g), and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride(4.22 g) in dichloromethane-N,N-dimethylformamide (1:1, 40 ml) wasstirred at room temperature for 12 hours. The reaction mixture wasdiluted with ethyl acetate, washed with aqueous sodiumhydrogencarbonate, with brine, and dried over magnesium sulfate. Afterthe solvent was evaporated, the residue was subjected to columnchromatography (silica gel chloroform-methanol) to give Object Compoundas a colorless crystal (185 mg).

mp: 51-52° C.; MASS (m/z): 193 (M+H)⁺ ; NMR (CDCl₃, δ): 2.50 (6H, s),3.01 (3H, d, J=6 Hz), 3.48 (2H, s), 6.16 (1H, br s), 7.38 (2H, d, J=8Hz), 7.72 (2H, d, J=8 Hz)

Preparation 33

To a suspension of lithium aluminum hydride (56 mg) in anhydroustetrahydrofuran (2 ml) was added Starting Compound (180 mg) at 0° C. Themixture was heated to reflux for 1.5 hours. The mixture was allowed tocool to room temperature and diluted with ether. To this mixture wasadded water (56 mg), 15% aqueous sodium hydroxide (56 mg), and water(110 mg). Filtration followed by evaporation of the solvent affordedObject Compound (125 mg) as a colorless oil.

MASS (m/z): 179 (M+H)⁺ ; NMR (CDCl₃, δ): 2.23 (6H, s), 2.45 (3H, s),3.40 (2H, s), 3.73 (2H, s), 7.27 (4H, s)

Preparation 34

The following object compound was obtained according to a similar mannerto that of Preparation 6.

MASS (FAB) (m/z): 478 (M+H)⁺ ; NMR (CDCl₃, δ): 1.28 (3H, t, J=8 Hz),1.39 (9H, s), 2.45-2.61 (4H, m), 2.76 (1H, dd, J=15, 5 Hz), 3.13 (1H,dd, J=15, 5 Hz), 3.20 (2H, s), 3.43-3.50 (2H, m), 3.60-3.64 (2H, m),4.08-4.22 (2H, m), 4.56-4.62 (1H, m), 5.17 (2H, q, J=8 Hz), 5.80 (1H, d,J=8 Hz), 7.33 (5H, br s)

Preparation 35

The following object compound was obtained according to a similar mannerto that of Preparation 10.

MASS (FAB) (m/z): 387 (M+H)⁺ ; NMR (CDCl₃, δ): 1.26 (3H, t, J=8 Hz),1.39 (9H, s), 2.50-3.90 (5H, m), 3.04-3.12 (1H, m), 3.23 (2H, s),3.52-3.62 (3H, m), 3.68-3.80 (1H, m), 4.18 (2H, q, J=8 Hz), 4.38-4.50(1H, m), 5.94 (1H, br s)

Preparation 36

Starting Compound (573 mg) was dissolved in a mixture of hydrochloricacid (1 ml) and methanol (5 ml), and stirred at 50° C. for 1 hour. Thereaction mixture was evaporated and the remaining solid was dried invacuo. To this solid was added dichloromethane (5 ml), Boc--Phe--OH (531mg), 1-hydroxybenzotriazole (284 mg) and1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (416 mg),and the mixture was stirred at room temperature for 12 hours. Themixture was diluted with ethyl acetate, washed with aqueous sodiumhydrogencarbonate, washed with brine, and dried over magnesium sulfate.Evaporation of the solvent followed by subjecting to columnchromatography (silica gel, chloroform-methanol) afforded ObjectCompound (820 mg) as a colorless oil.

MASS (m/z): 427 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (9H, s), 2.63 (2/3×3H, s),2.80 (1/3×3H, s), 3.0-3.1 (2H, m), 3.70 (1/3×3H, s), 3.90 (2/3×3H, s),4.19 (1/3×1H, d, J=17 Hz), 4.38 (1/3×1H, d, J=17 Hz), 4.53 (2/3×2H, ABq,Δ=0.11, J=15 Hz), 4.8-4.9 (1H, m), 5.30 (1/3×1H, br d, J=8 Hz), 5.38(2/3×1H, br d, J=8 Hz), 6.9-7.3 (7H, m), 7.9-8.0 (2H, m)

Preparation 37

The following object compound was obtained according to a similar mannerto that of Preparation 36.

MASS (m/z): 387 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.61 (3/4×3H, s),2.79 (1/4×3H, z), 2.93-3.03 (2H, m), 4.05 (1/4×1H, d, J=17 Hz), 4.32(1/4×1H, d, J=17 Hz), 4.45 (3/4×2H, ABq, Δ=0.12, J=15 Hz), 4.78-5.00(1H, m), 5.30-5.45 (1H, m), 6.80-7.30 (9H, m)

Preparation 38

Starting Compound (4.09 g) was dissolved in tetrahydrofuran (45 ml) andcooled to -15° C. N-Methyl-morpholine (1.1 ml) and isobutylchloroformate(1.38 g) were added successively to the solution, and stirred at thetemperature for 3 minutes. N-Methyl benzylamine (1.22 g) intetrahydrofuran (5 ml) was added to the mixture, and the whole wasstirred at 0° C. for 30 minutes. The reaction mixture was diluted withchloroform, washed with aqueous sodium hydrogencarbonate, washed withbrine, and dried over magnesium sulfate. Evaporation of the solvent gaveObject Compound (5.13 g) as white powder.

NMR (CDCl₃, δ): 1.40 (9H, s), 2.42 (3H, s), 2.72-3.04 (2H, m), 2.83(1/3×3H, s), 2.88 (2/3×3H, s), 4.30-4.65 (2H, m), 4.85-5.04 (1H, m),5.32-5.50 (1H, m), 7.00-7.95 (11H, m)

Preparation 39

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11 or 38.

(1) NMR (CDCl₃, δ): 1.40 (9H, s), 2.80 (3/4×3H, s), 2.85 (1/4×3H, s),4.33 (1/4×1H, d, J=15 Hz), 4.55 (1/4×1H, d, J=15 Hz), 4.60 (3/4×2H, ABq,Δ=0.10, J=14 Hz), 5.59 (3/4×1H, d, J=8 Hz), 5.62 (1/4×1H, d, J=8 Hz),6.05 (1H, d, J=8 Hz), 6.9-7.4 (10H, m)

(2) MASS (m/z): 389 (M+H)⁺ ; NMR (CDCl₃, δ): 2.93-3.22 (2H, m), 4.32(2H, d, J=16 Hz), 4.33-4.47 (1H, m), 5.06 (2H, s), 5.33 (1H, br s), 5.92(1H, br s), 6.98-7.41 (15H, m)

(3) MASS (m/z): 279 (M+H)⁺ ; NMR (CDCl₃, δ): 1.43 (2/5×9H, s), 1.48(3/5×9H, s), 2.88 (3/5×3H, s), 2.99 (2/5×3H, s), 3.95-4.08 (2H, m), 4.46(2/5×2H, s), 4.61 (3/5×2H, s), 5.50-5.62 (1H, br s), 7.10-7.42 (5H, m)

(4) MASS (m/z): 399 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.60 (2/3×3H,s), 2.78 (1/3×3H, s), 2.95-3.02 (2H, m), 3.76 (1/3×3H, s), 3.79 (2/3×3H,s), 3.98 (1/3×1H, d, J=17 Hz), 4.30 (1/3×1H, d, J=17 Hz), 4.42 (2/3×2H,ABq, Δ=0.13, J=15 Hz), 4.8-5.0 (1H, m), 5.33 (1/3×1H, br d, J=9 Hz),5.40 (2/3×1H, br d, J=9 Hz), 6.78 (1/3×2H, d, J=9 Hz), 6.80 (2/3×2H, d,J=9 Hz), 6.88 (1/3×2H, d, J=9 Hz), 7.03 (2/3×2H, d, J=9 Hz), 7.1-7.3(5H, m)

(5) MASS (m/z): 475 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (1/4×9H, s), 1.43(3/4×9H, s), 2.60 (3/4×3H, s), 2.81 (1/4×3H, s), 2.88-2.98 (2H, m), 4.22(1/4×2H, ABq, Δ=0.24, J=17 Hz), 4.48 (3/4×2H, ABq, Δ=0.13, J=15 Hz),4.75-4.88 (1H, m), 5.01 (3/4×2H, s), 5.05 (1/4×2H, s), 5.26-5.44 (1H,m), 6.77-7.45 (14H, m)

(6) MASS (m/z): 383 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.45-2.98(4H, m), 2.60 (3/5×3H, s), 2.80 (2/5×3H, s), 3.10-3.63 (2H, m),4.68-4.85 (1H, m), 5.25 (2/5×1H, br d, J=9 Hz), 5.35 (3/5×1H, br d, J=9Hz), 7.02-7.32 (10H, m)

(7) MASS (m/z): 419 (M+H)⁺ ; NMR (CDCl₃, δ): 1.41 (9H, s), 2.66 (3/4×3H,s), 2.87 (1/4×3H, s), 3.02 (2H, m), 4.24 (1/4×1H, d, J=17 Hz), 4.53(1/4×1H, d, J=17 Hz), 4.67 (3/4×2H, ABq, Δ=0.09, J=15 Hz), 4.9-5.0 (1H,m), 5.40 (1/4×1H, d, J=9 Hz), 5.46 (3/4×1H, d, J=9 Hz), 7.0-7.3 (6H, m),7.4-7.9 (6H, m)

(8) MASS (m/z): 419 (M+H)⁺ ; NMR (CDCl₃, δ): 1.38 (1/4×9H, s), 1.43(3/4×9H, s), 2.60 (3/4×3H, s), 2.90 (1/4×3H, s), 2.93-3.08 (2H, m), 4.63(1/4×2H, ABq, Δ=0.20, J=17 Hz), 4.80-4.98 (1H, m), 5.00 (3/4×2H, ABq,Δ=0.16, J=15 Hz), 5.32-5.50 (1H, m), 6.90-8.10 (12H, m)

(9) MASS (m/z): 411 (M⁺); NMR (CDCl₃, δ): 1.40 (9H, s), 2.59 (2/3×3H,s), 2.80 (1/3×3H, s), 2.93 (6H, s), 2.98 (2H, m), 3.95 (1/3×1H, d, J=17Hz), 4.30 (1/3×1H, d, J=17 Hz), 4.39 (2/3×2H, ABq, Δ=0.08, J=15 Hz),4.7-4.8 (2/3×1H, m), 4.9-5.0 (1/3×1H, m), 5.38 (1/3×1H, d, J=9 Hz), 5.43(2/3×1H, d, J=9 Hz), 6.63 (2H, d, J=8 Hz), 6.8-7.3 (7H, m)

(10) MASS (m/z): 426 (M+H)⁺ ; NMR (CDCl₃, δ): 1.39 (1/3×9H, s), 1.42(2/3×9H, s), 2.20 (1/3×6H, s), 2.22 (2/3×6H, s), 2.61 (2/3×3H, s), 2.82(1/3×3H, s), 2.92-3.04 (2H, m), 3.37 (1/3×2H, s), 3.39 (2/3×2H, s), 4.08(1/3×1H, d, J=17 Hz), 4.34 (1/3×1H, d, J=17 Hz), 4.48 (2/3×2H, ABq,Δ=0.10, J=15 Hz), 4.80-4.95 (1H, m), 5.30-5.45 (1H, m), 6.88-7.30 (9H,m)

(11) MASS (m/z): 381 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.25-2.42(1H, m), 2.65-2.80 (1H, m), 2.90-3.20 (2H, m), 3.48-3.90 (2H, m), 3.96(1/3×1H, d, J=17 Hz), 4.48 (1/3×1H, d, J=17 Hz), 4.65 (2/3×2H, ABq,Δ=0.19, J=17 Hz), 4.85-5.00 (1H, m), 5.38-5.52 (1H, m), 6.80-7.22 (9H,m)

(12) mp: 100-101° C.; MASS (m/z): 403 (M+H)⁺ ; NMR (CDCl₃, δ): 1.43 (9H,s), 2.62 (3/4×3H, s), 2.78 (1/4×3H, s), 2.90-3.10 (2H, m), 4.19 (1/4×2H,ABq, Δ=0.21, J=17 Hz), 4.45 (3/4×2H, ABq, Δ=0.12, J=15 Hz), 4.78-4.92(1H, m), 5.32 (1/4×1H, d, J=9 Hz), 5.38 (3/4×1H, d, J=9 Hz), 6.80-7.05(2H, m), 7.09-7.32 (7H, m)

(13) MASS (m/z): 447, 449 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.62(3/4×3H, s), 2.79 (1/4×3H, s), 2.90-3.08 (2H, m), 4.17 (1/4×2H, ABq,Δ=0.21, J=17 Hz), 4.42 (3/4×2H, ABq, Δ=0.12, J=15 Hz), 4.78-4.93 (1H,m), 5.25-5.42 (1H, m), 6.73-7.00 (2H, m), 7.08-7.45 (7H, m)

(14) MASS (m/z): 400 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (9H, s), 2.59(3/4×3H, s), 2.75 (1/4×3H, s), 2.90-3.08 (2H, m), 3.90 (1/4×3H, s), 3.93(3/4×3H, s), 4.34 (1/4×2H, ABq, Δ=0.10, J=17 Hz), 4.40 (3/4×2H, ABq,Δ=0.11, J=15 Hz), 4.74-5.05 (1H, m), 5.30-5.45 (1H, m), 6.55-6.70 (1H,m), 7.03-7.38 (6H, m), 7.80-8.00 (1H, m)

(15) NMR (CDCl₃, δ): 0.95 (3/5×3H, t, J=7.5 Hz), 1.02 (2/5×3H, t, J=7.5Hz), 1.40 (2/5×9H, s), 1.42 (3/5×9H, s), 2.85-3.55 (4H, m), 4.19(2/5×2H, ABq, Δ=0.18, J=17 Hz), 4.33 (3/5×1H, d, J=15 Hz), 4.73 (3/5×1H,d, J=15 Hz), 4.75-4.92 (1H, m), 5.25-5.42 (1H, m), 6.93-7.35 (10H, m)

(16) MASS (m/z): 404 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.63(5/6×3H, s), 2.76 (1/6×3H, s), 2.88-3.09 (2H, m), 4.04 (1/6×1H, d, J=17Hz), 4.30 (1/6×1H, d, J=17 Hz), 4.44 (5/6×2H, ABq, Δ=0.08, J=15 Hz),4.76-4.92 (1H, m), 5.22-5.38 (1H, m), 7.03-7.40 (7H, m), 8.05 (1/6×1H,d, J=2 Hz), 8.18 (5/6×1H, d, J=2 Hz)

(17) MASS (m/z): 384 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.51(1/5×3H, s), 2.53 (4/5×3H, s), 2.60 (4/5×3H, s), 2.78 (1/5×3H, s),2.90-3.06 (2H, m), 3.98 (1/5×1H, d, J=17 Hz), 4.32 (1/5×1H, d, J=17 Hz),4.44 (4/5×2H, ABq, Δ=0.06, J=15 Hz), 4.75-4.98 (1H, m), 5.25-5.42 (1H,m), 6.98-7.33 (7H, m), 8.18 (1/5×1H, d, J=2 Hz), 8.31 (4/5×1H, d, J=2Hz)

(18) MASS (m/z): 436 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.67(3/4×3H, s), 2.82 (1/4×3H, s), 2.95-3.07 (2H, m), 4.26 (1/4×2H, ABq,Δ=0.22, J=17 Hz), 4.53 (3/4×2H, s), 4.82-4.95 (1H, m), 5.28-5.42 (1H,m), 7.00-7.32 (7H, m), 7.50-7.62 (2H, m), 8.10 (1H, s), 8.52 (1H, s)

(19) MASS (m/z): 404 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.61(5/6×3H, s), 2.78 (1/6×3H, s), 2.92-3.08 (2H, m), 3.96 (1/6×1H, d, J=17Hz), 4.38 (1/6×1H, d, J=17 Hz), 4.47 (5/6×2H, ABq, Δ=0.07, J=15 Hz),4.76-4.92 (1H, m), 5.25-5.40 (1H, m), 7.10-7.35 (5H, m), 7.50 (1H, s),8.12 (1/6×1H, s), 8.28 (5/6×1H, s), 8.48 (1H, s)

(20) MASS (m/z): 370 (M+H)⁺ ; NMR (CDCl₃, δ): 1.38 (1/3×9H, s), 1.42(2/3×9H, s), 2.77 (2/3×3H, s), 2.89 (1/3×3H, s), 2.90-3.10 (2H, m), 4.38(1/3×2H, ABq, Δ=0.10, J=17 Hz), 4.61 (2/3×2H, s), 4.81-4.97 (1H, m),5.25-5.44 (1H, m), 6.87-7.67 (8H, m), 8.43-8.57 (1H, m)

(21) MASS (m/z): 370 (M+H)⁺ ; NMR (CDCl₃, δ): 1.39 (1/4×9H, s), 1.42(3/4×9H, s), 2.69 (3/4×3H, s), 2.82 (1/4×3H, s), 2.90-3.12 (2H, m), 4.28(1/4×2H, s), 4.48 (3/4×2H, ABq, Δ=0.06, J=15 Hz), 4.68-4.98 (1H, m),5.20-5.40 (1H, m), 6.73-7.35 (7H, m), 8.40-8.52 (2H, m)

(22) MASS (m/z): 370 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (1/5×9H, s), 1.42(4/5×9H, s), 2.63 (4/5×3H, s), 2.79 (1/5×3H, s), 2.92-3.06 (2H, m), 4.08(1/5×1H, d, J=17 Hz), 4.35 (1/5×1H, d, J=17 Hz), 4.49 (4/5×2H, ABq,Δ=0.09, J=15 Hz), 4.79-4.98 (1H, m), 5.28-5.42 (1H, m), 7.10-7.35 (7H,m), 8.28 (1/5×1H, s), 8.42 (4/5×1H, s), 8.50-8.55 (1H, m)

(23) MASS (m/z): 399 (M⁺ +1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.59(3H×2/3, s), 2.78 (3H×1/3, s), 2.98 (2H, d, J=7 Hz), 3.78 (3H, s), 3.99(1H×1/3, d, J=15 Hz), 4.31 (1H×1/3, d, J=15 Hz), 4.35 (1H×2/3, d, J=15Hz), 4.48 (1H×2/3, d, J=15 Hz), 4.83 (1H, m), 5.40 (1H, m), 6.80-7.04(4H, m), 7.16-7.25 (5H, m)

(24) MASS (ESI)(m/z): 383 (M+H)⁺ ; NMR (CDCl₃, 1δ): 1.42 (9H, s), 2.32(3H, s), 2.59 (3×2/3H, s), 2.83 (3×1/3H, s), 2.90-3.06 (2H, m),4.02-4.53 (2H, m), 4.82-4.96 (1H, m), 5.40-5.50 (1H, m), 6.88 (2×1/3H,d, J=8 Hz), 6.99 (2×2/3H, d, J=8 Hz), 7.05-7.10 (2H, m), 7.13-7.30 (5H,m)

(25) MASS (m/z): 309 (M⁺ +1); NMR (CDCl₃, δ): 1.38 (9H×1/3, s), 1.45(9H×2/3, s), 2.93 (3H×1/3, s), 3.05 (3H×2/3, s), 3.26 (1H×2/3, m), 3.44(1H×1/3, m), 3.67-3.88 (2H, m), 4.60-4.71 (3H, m), 5.70 (1H, m),7.17-7.38 (5H, m)

(26) MASS (m/z): 335 (M⁺ +1); NMR (CDCl₃, δ): 0.84 (6H×2/7, t, J=7 Hz),0.94 (3H×5/7, d, J=7 Hz), 1.00 (3H×5/7, d, J=7 Hz), 1.45 (9H, s),1.34-1.76 (3H, m), 2.92 (3H×2/7, s), 2.97 (3H×5/7, s), 4.48 (1H×5/7, d,J=15 Hz), 4.67 (1H×5/7, d, J=15 Hz), 4.65-4.72 (2H×2/7, m), 5.19(1H×2/7, d, J=7 Hz), 5.28 (1H×5/7, d, J=7 Hz), 7.20-7.34 (5H, m)

(27) MASS (m/z): 437 (M⁺ +1); NMR (CDCl₃, δ): 1.40 (9H×1/3, s), 1.45(9H×2/3, s), 2.67 (3H×2/3, s), 2.83 (3H×1/3, s), 3.02 (2H, d, J=8 Hz),4.22 (1H×1/3, d, J=15 Hz), 4.37 (1H×1/3, d, J=15 Hz), 4.50 (1H×2/3, d,J=15 Hz), 4.58 (1H×2/3, d, J=15 Hz), 4.90 (1H, m), 5.36 (1H, m),7.02-7.28 (7H, m), 7.53 (2H, d, J=8 Hz)

(28) MASS (m/z): 369 (M⁺ +1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.62(3H×2/3, s), 2.82 (3H×1/3, s), 3.00 (2H, d, J=7 Hz), 4.11 (1H×1/3, d,J=15 Hz), 4.36 (1H×1/3, d, J=15 Hz), 4:43 (1H×2/3, d, J=15 Hz), 4.54(1H×2/3, d, J=15 Hz), 4.86 (1H, m), 5.41 (1H, m), 6.96-7.28 (10H, m)

Preparation 40

Starting Compound (801 mg) was dissolved in dichloromethane (10 ml).Boron tribromide solution in dichloromethane (0.43 ml) was added to theabove solution at room temperature, and the whole was stirred at thesame temperature for 12 hours. Water (5 ml) was added to the mixture andstirred for 30 minutes. The mixture was neutralized by adding aqueoussodium hydrogencarbonate and then extracted three times with chloroform.The organic layer was dried over potassium carbonate. Evaporation of thesolvent gave Object Compound (406 mg) as an oil.

MASS (m/z): 285 (M+H)⁺ ; NMR (CDCl₃, δ): 2.74 (2/3×3H, s), 2.75-2.85(1H, m), 2.90 (1/3×3H, s), 3.00-3.10 (1H, m), 3.92 (1/3×1H, d, J=17 Hz),3.95-4.05 (1H, m), 4.10 (2/3×1H, d, J=15 Hz), 4.34 (1/3×1H, d, J=17 Hz),4.82 (2/3×1H, d, J=15 Hz), 6.60-7.35 (9H, m)

Preparation 41

Starting Compound (2.56 g) was dissolved in dichloromethane (5 ml) andcooled to 0° C. Trifluoroacetic acid (5 ml) was added to the solutionand the mixture was stirred at 0° C. for 3 hours. Aqueous sodiumhydroxide was added to the solution with ice-cooling to make basic, andthe solution was extracted three times with chloroform. The organiclayer was washed with brine and dried over magnesium sulfate.Evaporation of the solvent gave Object Compound (2.02 g) as an oil.

MASS (m/z): 413 (M+H)⁺ ; NMR (CDCl₃, δ): 2.43 (3H, s), 2.61-2.75 (1H,m), 2.80-2.95 (4H, m), 3.98-4.18 (1H, m), 4.33 (1/3×1H, d, J=17 Hz),4.57 (2/3×2H, ABq, Δ=0.16, J=15 Hz), 4.61 (1/3×1H, d, J=17 Hz),7.00-7.43 (11H, m), 7.75-7.97 (3H, m)

Preparation 42

The following object compounds were obtained according to a similarmanner to- that of Preparation 31 4 or 8.

(1) MASS (m/z): 255 (M+H)⁺ ; NMR (CDCl₃, δ): 2.75 (2/3×3H, s), 2.95(1/3×3H, s), 4.22 (1/3×1H, d, J=17 Hz), 4.58 (1/3×1H, d, J=17 Hz), 4.63(2/3×2H, ABq, Δ=0.09, J=15 Hz), 4.74 (1/3×1H, s), 4.77 (2/3×1H, s),6.92-7.45 (10H, m)

(2) NMR (CDCl₃, δ): 2.70 (3/5×3H, s), 2.72-2.85 (1H, m), 2.89 (2/5×3H,s), 2.93 (6H, s), 2.95-3.05 (1H, m), 3.90-4.00 (1H, m), 4.08 (2/5×1H, d,J=17 Hz), 4.35 (2/5×1H, d, J=17 Hz), 4.48 (3/5×2H, ABq, Δ=0.11, J=15Hz), 6.62-7.33 (9H, m)

(3) MASS (m/z): 326 (M+H)⁺ ; NMR (CDCl₃, δ): 2.23 (6 H, s), 2.71(3/5×3H, s), 2.72-2.85 (1H, m), 2.91 (2/5×3H, s), 2.92-3.05 (1H, m),3.41 (2H, s), 3.88 (2/5×1H, t, J=7 Hz), 3.97 (3/5×1H, t, J=7 Hz), 4.28(2/5×2H, ABq, Δ=0.21, J=17 Hz), 4.55 (3/5×2H, ABq, Δ=0.16, J=15 Hz),6.95-7.34 (9H, m)

(4) MASS (m/z): 281 (M+H)⁺ ; NMR (CDCl₃, δ): 2.42-3.06 (4H, m),3.22-3.88 (2H, m), 3.97-4.05 (1H, m), 4.14 (1/3×1H, d, J=17 Hz), 4.52(1/3×1H, d, J=17 Hz), 4.71 (2/3×2H, ABq, Δ=0.12, J=17 Hz), 6.88-7.32(9H, m)

(5) MASS (m/z): 303 (M+H)⁺ ; NMR (CDCl₃, δ): 2.70 (3/4×3H, s), 2.73-3.08(2H, m), 2.89 (1/4×3H, s), 3.80-4.02 (1H, m), 4.25 (1/4×2H, ABq, Δ=0.17,J=17 Hz), 4.50 (3/4×2H, ABq, Δ=0.21, J=15 Hz), 6.88-7.34 (9H, m)

(6) MASS (m/z): 347, 349 (M+H)⁺ ; NMR (CDCl₃, δ): 2.70 (3/4×3H, s),2.73-3.08 (2H, m), 2.89 (1/4×3H, s), 3.79-4.02 (1H, m), 4.23 (1/4×2H,ABq, Δ=0.17, J=17 Hz), 4.39 (3/4×1H, d, J=15 Hz), 4.59 (3/4×1H, d, J=15Hz), 6.82-7.45 (9H, m)

(7) MASS (m/z): 287 (M+H)⁺ ; NMR (CDCl₃, δ): 2.70 (3/4×3H, s), 2.73-3.08(2H, m), 2.88 (1/4×3H, s), 3.84-4.02 (1H, m), 4.25 (1/4×2H, ABq, Δ=0.20,J=17 Hz), 4.52 (3/4×2H, ABq, Δ=0.20, J=17 Hz), 6.90-7.35 (9H, m)

(8) MASS (m/z): 300 (M+H)⁺ ; NMR (CDCl₃, δ): 2.69 (3/4×3H, s), 2.74-3.10(2H, m), 2.87 (1/4×3H, s), 3.88-3.98 (1H, m), 3.93 (3H, s), 4.20(1/4×2H, ABq, Δ=0.25, J=17 Hz), 4.44 (3/4×2H, ABq, Δ=0.20, J=15 Hz),6.64-6.72 (1H, m), 7.10-7.45 (8H, m), 7.85-8.02 (1H, m)

(9) MASS (m/z): 283 (M+H)⁺ ; NMR (CDCl₃, δ): 1.03 (1/2×3H, t, J=7 Hz),1.07 (1/2×3H, t, J=7 Hz), 2.70-3.25 (3H+1/2×1H, m), 3.50-3.97(1H+1/2×1H, m), 4.22 (1/2×2H, ABq, Δ=0.13, J=17 Hz), 4.33 (1/2×1H, d,J=15 Hz), 4.80 (1/2×1H, d, J=15 Hz), 7.00-7.39 (10H, m)

(10) MASS (m/z): 303 (M+H)⁺ ; NMR (CDCl₃, δ): 2.49 (5/6×3H, s), 2.72(1/6×3H, s), 2.98-3.23 (2H, m), 3.70 (1/6×1H, d, J=17 Hz), 4.23 (1/6×1H,d, J=17 Hz), 4.40 (1H, t, J=7 Hz), 4.42 (5/6×2H, ABq, Δ=0.07, J=15 Hz),7.08-7.52 (7H, m), 8.06 (1/6×1H, d, J=2 Hz), 8.20 (5/6×1H, d, J=2 Hz)

(11) MASS (m/z): 284 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53 (3H, s), 2.70(3/4×3H, s), 2.73-3.08 (2H, m), 2.88 (1/4×3H, s), 3.84-4.02 (1H, m),4.12 (1/4×1H, d, J=17 Hz), 4.37 (1/4×1H, d, J=17 Hz), 4.51 (3/4×2H, ABq,Δ=0.17, J=15 Hz), 7.02-7.45 (7H, m), 8.26 (1/4×1H, s), 8.34 (3/4×1H, s)

(12) MASS (m/z): 336 (M+H)⁺ ; NMR (CDCl₃, δ): 2.72 (2/3×3H, s),2.72-3.10 (2H, m), 2.91 (1/3×3H, s), 3.88 (1/3×1H, t, J=7 Hz), 4.01(2/3×1H, t, J=7 Hz), 4.34 (1/3×2H, ABq, Δ=0.17, J=17 Hz), 4.60 (2/3×2H,ABq, Δ=0.16, J=15 Hz), 7.08-7.37 (7H, m), 7.53-7.65 (2H, m), 8.09 (1H,s), 8.52 (1H, s)

(13) MASS (m/z): 304 (M+H)⁺ ; NMR (CDCl₃, δ): 2.70 (5/6×3H, s),2.78-3.08 (2H, m), 2.88 (1/6×3H, s), 3.84 (1/6×1H, t, J=7 Hz), 3.97(5/6×1H, t, J=7 Hz), 4.28 (1/6×2H, ABq, Δ=0.22, J=17 Hz), 4.52 (5/6×2H,ABq, Δ=0.24, J=15 Hz), 7.10-7.36 (5H, m), 7.54 (1H, s), 8.22 (1/6×1H,s), 8.32 (5/6×1H, s), 8.50 (1H, s)

(14) MASS (m/z): 270 (M+H)⁺ ; NMR (CDCl₃, δ): 2.71 (3/4×3H, s),2.76-3.10 (2H, m), 2.88 (1/4×3H, s), 3.82-4.02 (1H, m), 4.28 (1/4×2H,ABq, Δ=0.20, J=17 Hz), 4.55 (3/4×2H, ABq, Δ=0.21, J=15 Hz), 7.11-7.55(7H, m), 8.32-8.58 (2H, m)

(15) NMR (CDCl₃, δ): 2.69 (3H×2/3, s), 2.78 (1H, m), 2.89 (3H×1/3, s),2.97 (1H, m), 3.78 (3H, s), 3.93 (1H, m), 4.10 (1H×1/3, d, J=15 Hz),4.35 (1H×1/3, d, J=15 Hz), 4.40 (1H×2/3, d, J=15 Hz), 4.57 (1H×2/3, d,J=15 Hz), 6.81-6.85 (2H, m), 6.94-7.29 (7H, m)

(16) MASS (ESI) (m/z): 283 (M+H)⁺ ; NMR (CDCl₃, δ): 2.32 (3H, s), 2.68(3×2/3H, s), 2.73-2.81 (1H, m), 2.89 (3×1/3H, s), 2.94-3.02 (1H, m),3.82-4.00 (1H, m), 4.12 (2×1/4H, d, J=16 Hz), 4.37 (2×1/4H, d, J=16 Hz),4.43 (2×1/4H, d, J=15 Hz), 4.58 (2×1/4H, d, J=15 Hz), 6.92 (1H, d, J=8Hz), 7.02-7.31 (8H, m)

(17) NMR (CDCl₃, δ): 2.68 (3H×2/7, s), 2.85 (3H×5/7, s), 3.92-4.61 (4H,m), 4.86 (1H, br s), 7.11-7.20 (5H, m), 8.30 (2H, br s)

(18) NMR (CDCl₃, δ): 0.86 (6H×2/9, t, J=7 Hz), 0.96 (3H×7/9, d, J=7 Hz),1.02 (3H×7/9, d, J=7 Hz), 1.52 (1H, m), 2.05 (2H, m), 2.86 (3H×1/3, s),2.91 (3H×2/3, s), 3.95 (2H×1/2, s), 4.20 (1H×1/2, d, J=15 Hz), 4.62 (1H,m), 4.85 (1H×1/2, d, J=15 Hz), 7.18-7.34 (5H, m), 8.57 (2H, br s)

(19) NMR (CDCl₃, δ): 2.53 (3H×4/5, s), 2.80 (3H×1/5, s), 3.06 (1H, dd,J=8, 13 Hz), 3.32 (1H, dd, J=6, 13 Hz), 3.77 (1H×1/5, d, J=15 Hz), 4.31(1H×1/5, d, J=15 Hz), 4.54 (2H×4/5, s), 4.68 (1H, dd, J=6, 8 Hz),7.10-7.39 (7H, m), 7.56 (2H, t, J=8 Hz)

(20) NMR (CDCl₃, δ): 2.37 (3H×3/4, s), 2.65 (3H×1/4, s), 3.22 (1H, m),3.60 (1H, m), 3.60 (1H×1/4, d, J=16 Hz), 4.11 (1H×3/4, d, J=15 Hz), 4.28(1H×1/4, d, J=16 Hz), 4.67 (1H×3/4, d, J=15 Hz), 4.89 (1H, m), 6.98-7.26(10H, m), 8.77 (2H, br s)

Preparation 43

The following object compounds were obtained according to a similarmanner to that of Preparation 10.

(1) MASS (m/z): 482 (M⁺ -1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.60 (3H×2/3,s), 2.78 (3H×1/3, s), 2.72-3.16 (4H, m), 4.21 (1H×2/3, d, J=15 Hz), 4.23(1H×1/3, d, J=15 Hz), 4.31 (1H×1/3, d, J=15 Hz), 4.52 (1H, m), 4.67(1H×2/3, d, J=15 Hz), 5.22 (1H, m), 6.17 (1H, m), 6.82-7.25 (10H, m),7.99 (1H, d, J=8 Hz)

(2) MASS (m/z): 484 (M⁺ +1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.62 (1H, m),2.69 (3H×2/3, s), 2.78 (3H×1/3, s), 2.93-3.05 (3H, m), 4.23-4.33 (1H,m), 4.48-4.62 (2H, m), 5.14 (1H, m), 5.92-6.01 (1H, m), 6.92 (2H, m),7.06 (1H, m), 7.18-7.22 (7H, m), 7.83-7.94 (1H, m)

Preparation 44

1-tert-Butoxycarbonyl-4-ethylpiperazine (477 mg) was dissolved in amixture of hydrochloric acid (1 ml) and methanol (2 ml), and heated toreflux for 3 hours. The reaction mixture was allowed to cool to roomtemperature, evaporated, and dried in vacuo to give a white solid. Tothis solid was added dichloromethane (5 ml), Starting Compound (972 mg),1-hydroxybenzotriazole (278.1 mg), and triethylamine (0.3 ml). Themixture was cooled in ice, added1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (360 mg),then stirred at room temperature for 12 hours. The reaction mixture wasdiluted with ethyl acetate, washed with aqueous sodiumhydrogencarbonate, washed with brine, and dried over magnesium sulfate.Evaporation of the solvent followed by subjecting to columnchromatography (silica gel, chloroform-methanol) afforded ObjectCompound (961 mg) as a white powder.

MASS (m/z): 580 (M+H)⁺ ; NMR (CDCl₃, δ): 1.09 (3H, t, J=7 Hz), 1.48 (9H,s), 2.34-2.65 (7H, m), 2.54 (2/3×3H, s), 2.78 (1/3×3H, s), 2.93-3.30(3H, m), 3.40-3.68 (4H, m), 4.18 (1/3×2H, ABq, Δ=0.17, J=17 Hz), 4.30(2/3×1H, d, J=15 Hz), 4.45-4.60 (1H, m), 4.62 (2/3×1H, d, J=15 Hz),5.08-5.20 (1H, m), 5.97-6.11 (1H, m), 6.82-7.32 (10H, m), 7.32-7.50 (1H,m)

Preparation 45

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6 or 11.

(1) MASS (m/z): 566 (M⁺ 1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.30 (3H, s),2.35-2.45 (4H, m), 2.53 (3H×2/3, s), 2.60 (1H, m), 2.78 (3H×1/3, s),2.95-3.13 (2H, m), 3.22 (1H, m), 3.46 (2H, m), 3.61 (2H, m), 4.08(1H×1/3, d, J=15 Hz), 4.27 (1H×1/3, d, J=15 Hz), 4.29 (1H×2/3, d, J=15Hz), 4.52 (1H, m), 4.63 (1H×2/3, d, J=15 Hz), 5.12 (1H, m), 6.03 (1H, d,J=7 Hz), 6.87-7.04 (2H, m), 7.20-7.27 (8H, m), 7.38 (1H×1/3, d, J=8 Hz),7.45 (1H×2/3, d, J=8 Hz)

(2) MASS (m/z): 566 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.29 (3H, s),2.33-2.53 (5H, m), 2.58 (3H×2/3, s), 2.84 (3H×1/3, s), 2.94-3.21 (3H,m), 3.43 (2H, m), 3.59 (2H, m), 4.15 (1H×1/3, d, J=15 Hz), 4.30 (1H×1/3,d, J=15 Hz), 4.33 (1H×2/3, d, J=15 Hz), 4.54 (1H, m), 4.66 (1H×2/3, d,J=15 Hz), 5.13 (1H, m), 5.92-5.99 (1H, m), 6.94-7.29 (10H, m), 7.52 (1H,d, J=8 Hz)

(3) MASS (FAB) (m/z): 638 (M+H)⁺ ; NMR (CDCl₃, δ): 1.27 (3H, t, J=8 Hz),1.47 (9H, s), 2.53 (3×2/3H, s), 2.50-2.62 (5H, m), 2.78 (3×1/3H, s),2.95-3.13 (2H, m), 3.17-3.26 (1H, m), 3.22 (2H, s), 3.47-3.52 (2H, m),3.62-3.69 (2H, m), 4.08-4.32 (2×2/3H, m), 4.19 (2H, q, J=8 Hz),4.47-4.57 (1H, m), 4.62 (2×1/3H, d, J=15 Hz), 5.08-5.17 (1H, m), 6.02(1H, d, J=8 Hz), 6.85-6.89 (2×1/3H, m), 7.01-7.03 (2×2/3H, m), 7.16-7.30(8H, m), 7.40 (1×1/3H, d, J=8 Hz), 7.45 (1×2/3H, d, J=8 Hz)

Preparation 46

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11 or 38.

(1) MASS (m/z): 697 (M+H)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 2.42 (3H, s),2.48-2.62 (1H, m), 2.80-2.95 (1H, m), 2.82 (1/3×3H, s), 2.88 (2/3×3H,s), 2.95-3.10 (1H, m), 3.10-3.26 (1H, m), 3.35-3.72 (8H, m), 4.28-4.68(3H, m), 5.10-5.25 (1H, m), 5.94-6.06 (1H, m), 7.02-7.90 (12H, m)

(2) MASS (m/z): 552 (M+H)⁺ ; NMR (CDCl₃, δ): 1.44 (9H, s), 2.23-2.42(4H, m), 2.26 (3H, s), 2.45-2.70 (1H, m), 2.81 (2/3×3H, s), 2.85(1/3×3H, s), 3.00-3.25 (1H, m), 3.30-3.65 (4H, m), 4.32 (1/3×1H, d, J=17Hz), 4.42-4.61 (1H+1/3×1H, m), 4.60 (2/3×2H, ABq, Δ=0.16, J=15 Hz),5.73-5.87 (1H, m), 5.98-6.12 (1H, m), 6.90-7.47 (10H, m), 8.03-8.25 (1H,m)

(3) MASS (m/z): 569 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.50 (2/3×3H,s), 2.50-2.65 (1H, m), 2.74 (1/3×3H, s), 2.95-3.25 (3H, m), 3.38-3.70(8H, m), 3.77 (2/5×1H, d, J=17 Hz), 4.20 (2/5×1H, d, J=17 Hz), 4.35(3/5×2H, ABq, Δ=0.10, J=15 Hz), 4.48-4.62 (1H, m), 5.02-5.22 (1H, m),6.02 (1H, br d), 6.28 (2/3×1H, br s), 6.60-7.55 (10H+1/3×1H, m)

(4) MASS (m/z): 608 (M⁺); NMR (CDCl₃, δ): 1.46 (9H, s), 2.30 (3H, s),2.30-2.63 (5H, m), 2.50 (3/5×3H, s), 2.73 (2/5×3H, s), 2.90 (2/5×6H, s),2.92 (3/5×6H, s), 2.97-3.12 (2H, m), 3.12-3.30 (1H, m), 3.37-3.70 (4H,m), 3.87 (2/5×1H, d, J=17 Hz), 4.19 (2/5×1H, d, J=17 Hz), 4.22 (3/5×1H,d, J=15 Hz), 4.47-4.58 (1H, m), 4.50 (3/5×1H, d, J=15 Hz), 5.00-5.25(1H, m), 5.93-6.10 (1H, br d), 6.42-7.52 (10H, m)

(5) MASS (m/z): 623 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.23 (1/3×6H,s), 2.25 (2/3×6H, s), 2.30 (3H, s), 2.32-2.50 (4H, m), 2.50-2.64 (1H,m), 2.53 (2/3×3H, s), 2.78 (1/3×3H, s), 2.92-3.30 (3H, m), 3.39 (1/3×2H,s), 3.42 (2/3×2H, s), 3.42-3.70 (4H, m), 4.17 (1/3×2H, ABq, Δ=0.17, J=17Hz), 4.28 (2/3×1H, d, J=15 Hz), 4.43-4.60 (1H, m), 4.62 (2/3×1H, d, J=15Hz), 5.03-5.20 (1H, m), 5.96-6.10 (1H, m), 6.80-7.50 (10H, m)

(6) MASS (m/z): 578 (M+H)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 2.18-2.82(7H, m), 2.30 (3H, s), 2.92-3.12 (2H, m), 3.12-3.30 (1H, m), 3.37-3.85(6H, m), 3.89 (1/3×1H, d, J=17 Hz), 4.32 (1/3×1H, d, J=17 Hz), 4.45-4.58(1H, m), 4.62 (2/3×2H, ABq, Δ=0.15, J=17 Hz), 5.10-5.21 (1H, m),5.98-6.10 (1H, m), 6.78-7.57 (10H, m)

(7) MASS (m/z): 600 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.30 (3H, s),2.32-2.50 (4H, m), 2.52-2.63 (1H, m), 2.55 (2/3×3H, s), 2.75 (1/3×3H,s), 2.95-3.30 (3H, m), 3.38-3.68 (4H, m), 4.14 (1/3×2H, ABq, Δ=0.09,J=17 Hz), 4.22 (2/3×1H, d, J=15 Hz), 4.45-4.58 (1H, m), 4.58 (2/3×1H, d,J=15 Hz), 5.05-5.20 (1H, m), 5.95-6.10 (1H, m), 6.70-6.95 (2H, m),7.12-7.45 (8H, m)

(8) MASS (m/z): 644, 646 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.30(3H, s), 2.30-2.50 (4H, m), 2.50-2.63 (1H, m), 2.55 (3/4×3H, s), 2.75(1/4×3H, s), 2.90-3.30 (3H, m), 3.38-3.68 (4H, m), 4.13 (1/4×2H, ABq,Δ=0.07, J=17 Hz), 4.22 (3/4×1H, d, J=15 Hz), 4.46-4.59 (1H, m), 4.58(3/4×1H, d, J=15 Hz), 5.03-5.17 (1H, m), 5.97-6.08 (1H, m), 6.62-6.91(2H, m), 7.15-7.48 (8H, m)

(9) MASS (m/z): 584 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.30 (3H, s),2.30-2.48 (4H, m), 2.50-2.65 (1H, m), 2.54 (3/4×3H, s), 2.73 (1/4×3H,s), 2.92-3.30 (3H, m), 3.38-3.68 (4H, m), 4.13 (1/4×2H, ABq, Δ=0.14,J=17 Hz), 4.23 (3/4×1H, d, J=15 Hz), 4.45-4.59 (1H, m), 4.58 (3/4×1H, d,J=15 Hz), 5.05-5.18 (1H, m), 5.98-6.10 (1H, m), 6.72-7.03 (4H, m),7.15-7.48 (6H, m)

(10) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.30 (3H,s), 2.33-2.50 (4H, m), 2.50-2.63 (1H, m), 2.52 (3/4×3H, s), 2.71(1/4×3H, s), 2.95-3.28 (3H, m), 3.38-3.68. (4H, m), 3.89 (1/4×3H, s),3.92 (3/4×3H, s), 3.92 (1/4×1H, d, J=17 Hz), 4.18 (1/4×1H, d, J=17 Hz),4.20 (3/4×1H, d, J=15 Hz), 4.48-4.58 (1H, m), 4.51 (3/4×1H, d, J=15 Hz),5.01-5.27 (1H, m), 5.95-6.10 (1H, br d), 6.53-6.68 (1H, m), 7.12-7.48(7H, m), 7.74-7.94 (1H, m)

(11) MASS (m/z): 580 (M+H)⁺ ; NMR (CDCl₃, δ): 0.90 (3/5×3H, t, J=7 Hz),0.98 (2/5×3H, t, J=7 Hz), 1.45 (9H, s), 2.32 (3H, s), 2.35-2.62 (5H, m),2.83-3.32 (5H, m), 3.35-3.70 (4H, m), 4.12 (2/5×2H, ABq, Δ=0.18, J=17Hz), 4.18 (3/5×1H, d, J=15 Hz), 4.42-4.62 (1H, m), 4.78 (3/5×1H, d, J=15Hz), 4.96-5.18 (1H, m), 5.92-6.10 (1H, br d), 6.85-7.46 (11H, m)

(12) MASS (m/z): 601 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.30 (3H,s), 2.30-2.51 (4H, m), 2.51-2.63 (1H, m), 2.58 (4/5×3H, s), 2.73(1/5×3H, s), 2.93-3.30 (3H, m), 3.40-3.70 (4H, m), 4.16 (1/5×2H, ABq,Δ=0.09, J=17 Hz), 4.25 (4/5×1H, d, J=15 Hz), 4.48-4.58 (1H, m), 4.57(4/5×1H, d, J=15 Hz), 5.02-5.17 (1H, m), 5.97-6.10 (1H, m), 7.10-7.48(8H, m), 8.01 (1/5×1H, d, J=2 Hz), 8.15 (4/5×1H, d, J=2 Hz)

(13) MASS (m/z): 581 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.30 (3H,s), 2.30-2.64 (5H, m), 2.51 (1/4×3H, s), 2.53 (3/4×3H×2, s), 2.72(1/4×3H, s), 2.94-3.30 (3H, m), 3.39-3.68 (4H, m), 4.00 (1/4×1H, d, J=17Hz), 4.22 (1/4×1H, d, J=17 Hz), 4.27 (3/4×1H, d, J=15 Hz), 4.46-4.60(1H, m), 4.53 (3/4×1H, d, J=15 Hz), 5.01-5.21 (1H, m), 5.95-6.10 (1H, brd), 6.91-7.50 (8H, m), 8.14 (1/4×1H, d, J=2 Hz), 8.27 (3/4×1H, d, J=2Hz)

(14) MASS (m/z): 568 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.50-2.63(1H, m), 2.51 (1/4×3H, s), 2.53 (3/4×3H×2, s), 2.73 (1/4×3H, s),2.95-3.28 (3H, m), 3.38-3.78 (8H, m), 3.98 (1/4×1H, d, J=17 Hz), 4.23(1/4×1H, d, J=17 Hz), 4.28 (3/4×1H, d, J=15 Hz), 4.46-4.62 (1H, m), 4.54(3/4×1H, d, J=15 Hz), 5.01-5.22 (1H, m), 5.93-6.08 (1H, m), 6.95-7.52(8H, m), 8.15 (1/4×1H, s), 8.28 (3/4×1H, s)

(15) MASS (m/z): 633 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.30 (3H,s), 2.30-2.63 (5H, m), 2.61 (2/3×3H, s), 2.89 (1/3×3H, s), 2.93-3.30(3H, m), 3.37-3.68 (4H, m), 4.23 (1/3×2H, ABq, Δ=0.12, J=17 Hz), 4.38(2/3×1H, d, J=15 Hz), 4.45-4.60 (1H, m), 4.62 (2/3×1H, d, J=15 Hz),5.08-5.21 (1H, m), 5.95-6.10 (1H, m), 6.91-7.62 (10H, m), 8.11 (1H, s),8.52 (1H, s)

(16) MASS (m/z): 601 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.30 (3H,s), 2.30-2.50 (4H, m), 2.50-2.64 (1H, m), 2.56 (4/5×3H, s), 2.75(1/5×3H, s), 2.93-3.30 (3H, m), 3.40-3.68 (4H, m), 4.18 (1/5×2H, ABq,Δ=0.09, J=17 Hz), 4.22 (4/5×1H, d, J=15 Hz), 4.46-4.62 (1H, m), 4.64(4/5×1H, d, J=15 Hz), 5.02-5.15 (1H, m), 5.96-6.10 (1H, m), 7.10-7.52(7H, m), 8.08 (1/5×1H, s), 8.23 (4/5×1H, s), 8.41-8.50 (1H, m)

(17) MASS (m/z): 588 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.50-2.62(1H, m), 2.58 (3/4×3H, s), 2.73 (1/4×3H, s), 2.92-3.28 (3H, m),3.39-3.78 (8H, m), 4.15 (1/4×2H, ABq, Δ=0.13, J=17 Hz), 4.27 (3/4×1H, d,J=15 Hz), 4.48-4.61 (1H, m), 4.55 (3/4×1H, d, J=15 Hz), 5.02-5.15 (1H,m), 5.93-6.08 (1H, m), 6.92-7.50 (8H, m), 8.02 (1/4×1H, m), 8.15(3/4×1H, m)

(18) MASS (m/z): 554 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.48-2.62(1H, m), 2.55 (3/4×3H, s), 2.75 (1/4×3H, s), 2.92-3.28 (3H, m),3.35-3.80 (8H, m), 4.18 (1/4×2H, ABq, Δ=0.18, J=17 Hz), 4.29 (3/4×1H, d,J=15 Hz), 4.46-4.62 (1H, m), 4.61 (3/4×1H, d, J=15 Hz), 5.00-5.18 (1H,m), 5.93-6.07 (1H, m), 7.03-7.50 (8H, m), 8.18-8.53 (2H, m)

(19) MASS (m/z): 567 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.30 (3H,s), 2.32-2.48 (4H, m), 2.52-2.63 (1H, m), 2.54 (3/4×3H, s), 2.74(1/4×3H, s), 2.93-3.30 (3H, m), 3.38-3.68 (4H, m), 4.18 (1/4×2H, ABq,Δ=0.14, J=17 Hz), 4.28 (3/4×1H, d, J=15 Hz), 4.45-4.60 (1H, m), 4.62(3/4×1H, d, J=15 Hz), 5.03-5.20 (1H, m), 5.93-6.10 (1H, m), 7.00-7.50(8H, m), 8.18-8.53 (2H, m)

(20) MASS (m/z): 596 (M⁺ +1); NMR (CDCl₃, δ): 1.44 (9H, s), 2.28 (3H,s), 2.37 (4H, m), 2.51 (3H×2/3, s), 2.60-2.79 (1H, m), 2.73 (3H×1/3, s),2.95-3.07 (2H, m), 3.22 (1H, m), 3.46 (2H, m), 3.61 (2H, m), 3.77(3H×1/3, s), 3.78 (3H×2/3, s), 3.96 (1H×1/3, d, J=15 Hz), 4.22 (1H×2/3,d, J=15 Hz), 4.41 (1H×1/3, d, J=15 Hz), 4.54 (1H×2/3, d, J=15 Hz), 4.54(1H, m), 5.06-5.18 (1H, m), 6.02 (1H, m), 6.77-7.00 (4H, m), 7.08-7.25(5H, m), 7.43 (1H, m)

(21) MASS (ESI) (m/z): 580 (M+H)⁺ ; NMR (CDCl₃, δ): 1.43 (9H, s), 2.25(3H, s), 2.31 (3H, s), 2.35-2.48 (4H, m), 2.52 (3×2/3H, s), 2.54-2.62(1H, m), 2.76 (3×1/3H, s), 2.97-3.10 (2H, m), 3.17-3.28 (1H, m),3.42-3.50 (2H, m), 3.58-3.64 (2H, m), 4.02 (2×1/4H, d, J=16 Hz), 4.22(2×1/4H, d, J=16 Hz), 4.27 (2×1/4H, d, J=15 Hz), 4.58 (2×1/4H, d, J=15Hz), 4.48-4.57 (1H, m), 5.08-5.19 (1H, m), 6.03 (1H, d, J=8 Hz), 6.78(2×1/3H, d, J=8 Hz), 6.91 (2×2/3H, d, J=8 Hz), 7.03 (2H, t, J=8 Hz),7.18-7.30 (5H, m), 7.40 (1×1/3H, d, J=8 Hz), 7.47 (1×2/3H, d, J=8 Hz)

(22) MASS (m/z): 506 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.28 (3H,s), 2.35-2.42 (4H, m), 2.57 (1H, m), 2.93 (3H×1/3, s), 2.98 (3H×2/3, s),3.29-3.75 (6H, m), 3.86-3.94 (1H, m), 4.52 (1H×2/3, d, J=15 Hz), 4.54(1H, m), 4.63 (2H×1/3, s), 4.71 (1H×2/3, d, J=15 Hz), 5.02 (1H, m), 5.89(1H, d, J=8 Hz), 7.15-7.35 (5H, m), 7.53 (1H×1/3, d, J=8 Hz), 7.61(1H×2/3, d, J=8 Hz)

(23) MASS (m/z): 532 (M⁺ +1); NMR (CDCl₃, δ): 0.78 (3H×1/3, d, J=7 Hz),0.83 (3H×1/3, d, J=7 Hz), 0.92 (3H×2/3, d, J=7 Hz), 0.96 (3H×2/3, d, J=7Hz), 1.44 (9H, s), 1.43-1.70 (3H, m), 2.30 (3H, s), 2.38 (4H, m), 2.57(1H, m), 2.92 (3H×1/3, s), 2.97 (3H×2/3, s), 3.17 (1H, m), 3.46 (2H, m),3.59 (2H, m), 4.42 (1H×2/3, d, J=15 Hz), 4.53 (1H, m), 4.57 (1H×1/3, d,J=15 Hz), 4.69 (1H×1/3, d, J=15 Hz), 4.73 (1H×2/3 d, J=15 Hz), 4.96 (1H,m), 6.05 (1H, m), 7.17-7.35 (6H, m)

(24) MASS (m/z): 634 (M⁺ +1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.30 (3H,s), 2.35-2.46 (4H, m), 2.52-2.61 (1H, m), 2.59 (3H×3/4, s), 2.78(3H×1/4, s), 2.93-3.26 (3H, m), 3.45 (2H, m), 3.60 (2H, m), 4.27(2H×1/4, s), 4.33 (1H×3/4, d, J=15 Hz), 4.53 (1H, m), 4.65 (1H×3/4, d,J=15 Hz), 5.05 (1H×1/4, m), 5.14 (1H×3/4, q, J=7 Hz), 6.02 (1H, m),6.90-7.23 (7H, m), 7.33-7.52 (3H, m)

(25) MASS (m/z): 566 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.29 (3H,s), 2.33-2.53 (5H, m), 2.58 (3H×2/3, s), 2.84 (3H×1/3, s), 2.94-3.21(3H, m), 3.43 (2H, m), 3.59 (2H, m), 4.15 (1H×1/3, d, J=15 Hz), 4.30(1H×1/3, d, J=15 Hz), 4.33 (1H×2/3, d, J=15 Hz), 4.54 (1H, m), 4.66(1H×2/3, d, J=15 Hz), 5.13 (1H, m), 5.92-5.99 (1H, m), 6.94-7.29 (10H,m), 7.52 (1H, d, J=8 Hz)

(26) MASS (m/z): 574 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.54(3H×2/3, s), 2.71 (1H, m), 2.81 (3H×1/3, s), 2.92-3.12 (3H, m), 4.05(1H×1/3, d, J=15 Hz), 4.28 (1H×1/3, d, J=15 Hz), 4.32 (1H×2/3, d, J=15Hz), 4.53 (1H, m), 4.61 (1H×2/3, d, J=15 Hz), 5.07-5.18 (3H, m), 5.58(1H, m), 6.89-7.34 (16H, m)

(27) MASS (m/z): 574 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.59(3H×2/3, s), 2.68 (1H, dd, J=5, 16 Hz), 2.84 (3H×1/3, s), 2.95-3.05 (3H,m), 4.09 (1H×1/3, d, J=15 Hz), 4.31 (1H×1/3, d, J=15 Hz), 4.37 (1H×2/3,d, J=15 Hz), 4.53 (1H, m), 4.62 (1H×2/3, d, J=15 Hz), 5.07-5.17 (3H, m),5.56 (1H, m), 6.93-7.36 (16H, m)

Preparation 47

Starting Compound (194 mg) was dissolved in methanol (20 ml), andhydrogenated (3 kg/cm²) over 10% palladium on carbon (20 mg) at roomtemperature for 3 hours. The palladium on carbon was filtered off, andthe remaining solution was evaporated and dried in vacuo. The residuewas dissolved in dichloromethane (5 ml), and to this solution was addedCompound A (153 mg), 1-hydroxybenzotriazole (65 mg), and1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (104 mg)with ice-cooling, then the mixture was stirred at room temperature for15 hours. The reaction mixture was diluted with chloroform, washed withaqueous sodium hydrogencarbonate, washed with brine, and dried overmagnesium sulfate. Evaporation of the solvent followed by subjecting tocolumn chromatography (silica gel, chloroform-methanol) afforded ObjectCompound (173 mg) as white powder.

MASS (m/z): 539 (M+H)⁺ ; NMR (CDCl₃, δ): 1.36 (9H, s), 2.58-2.68 (1H,m), 2.90-3.00 (1H, m), 3.03-3.12 (1H, m), 3.25-3.45 (5H, m), 3.50-3.66(4H, m), 4.30-4.45 (3H, m), 4.60-4.72 (1H, m), 5.66 (1H, br d),6.72-6.90 (2H, m), 7.08-7.30 (10H, m)

Preparation 48

The following object compound was obtained according to a similar mannerto that of Preparation 47.

MASS (m/z): 449 (M+H)⁺ ; NMR (CDCl₃, δ): 1.39 (9H, s), 2.62-2.72 (1H,m), 2.87-3.14 (2H, m), 3.22-3.32 (1H, m), 3.40-3.47 (2H, m), 3.50-3.57(2H, m), 3.62-3.70 (4H, m), 4.37-4.50 (1H, m), 4.60-4.70 (1H, m), 5.31(1H, br s), 5.75 (1H, br d), 6.48 (12H, br d), 6.83 (1H, br d),7.20-7.35 (5H, m)

Preparation 49

Trifluoroacetic acid (4 ml) was added to Starting Compound (700 mg) withice-cooling, and stirred at room temperature for 1 hour. The reactionmixture was evaporated, and to the remaining oil was added hydrogenchloride in methanol and evaporated, then the remaining solid was driedin vacuo. To this solid was added dichloromethane (4 ml), Compound A(535 mg), 1-hydroxybenzotriazole (244 mg), and1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (322 mg), and the mixturewas stirred at room temperature for 12 hours. The reaction mixture wasdiluted with chloroform, washed with aqueous sodium hydrogencarbonate,washed with brine, and dried over magnesium sulfate. Evaporation of thesolvent followed by subjecting to column chromatography (silica gel,chloroform-methanol) afforded Object Compound (728 mg) as white powder.

MASS (m/z): 583 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.50 (2/3×3H, s),2.5-2.6 (1H, m), 2.73 (1/3×3H, s), 3.0-3.1 (2H, m), 3.1-3.2 (1H, m),3.4-3.7 (8H, m), 3.75 (1/3×3H, s), 3.78 (2/3×3H, s), 3.95 (1/3×1H, d,J=17 Hz), 4.22 (2/3×1H, d, J=15 Hz), 4.22 (1/3×1H, d, J=17 Hz), 4.54(2/3×1H, d, J=15 Hz), 4.5-4.6 (1H, m), 5.1-5.2 (1H, m), 6.00 (1H, br d,J=9 Hz), 6.7-6.8 (1/3×4H, m), 6.78 (2/3×2H, d, J=9 Hz), 6.98 (2/3×2H, d,J=9 Hz), 7.1-7.2 (5H, m), 7.40 (1/3×1H, d, J=8 Hz), 7.45 (2/3×1H, d, J=8Hz)

Preparation 50

The following object compounds were obtained according to a similarmanner to that of Preparation 49.

(1) MASS (m/z): 463 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45 (9H, s), 2.48-2.63(1H, m), 2.87 (2/3×3H, s), 2.98 (1/3×3H, s), 3.17-3.78 (9H, m),4.02-4.22 (3H, m), 4.47 (1/3×2H, s), 4.61 (2/3×2H, ABq, Δ=0.09, J=15Hz), 6.00-6.13 (1H, m), 7.10-7.70 (6H, m)

(2) MASS (m/z): 539 (M+H)⁺ ; NMR (CDCl₃, δ): 1.43 (9H, s), 2.5-2.6 (2H,m), 2.80 (2/3×3H, s), 2.85 (1/3×3H, s), 3.0-3.1 (1H, m), 3.3-3.6 (8H,m), 4.32 (1/3×1H, d, J=15 Hz), 4.42 (1/3×1H, d, J=15 Hz), 4.60 (2/3×2H,ABq, Δ=0.15, J=15 Hz), 5.78 (2/3×1H, d, J=7 Hz), 5.82 (1/3×1H, d, J=7Hz), 6.10 (1H, br d, J=7 Hz), 6.9-7.4 (10H, m), 8.12 (1H, br d, J=7 Hz)

(3) MASS (m/z): 659 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.48-2.62(1H, m), 2.54 (2/3×3H, s), 2.78 (1/3×3H, s), 2.90-3.05 (2H, m),3.10-3.28 (1H, m), 3.37-3.75 (8H, m), 4.10 (1/3×1H, d, J=17 Hz), 4.27(1/3×1H, d, J=17 Hz), 4.28 (2/3×1H, d, J=15 Hz), 4.46-4.60 (1H, m), 4.60(2/3×1H, d, J=15 Hz), 5.01 (2/3×2H, s), 5.02-5.13 (1H, m), 5.07 (1/3×2H,s), 6.00 (1H, br d), 6.75-7.48 (15H, m)

(4) MASS (m/z): 672 (M+H)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 2.29 (3H, s),2.30-2.49 (4H, m), 2.50-2.63 (1H, m), 2.54 (2/3×3H, s), 2.77 (1/3×3H,s), 2.85-3.10 (2H, m), 3.13-3.30 (1H, m), 3.35-3.68 (4H, m), 4.19(1/3×2H, ABq, Δ=0.16, J=17 Hz), 4.27 (2/3×1H, d, J=15 Hz), 4.42-4.62(1H, m), 4.62 (2/3×1H, d, J=15 Hz), 4.94-5.17 (3H, m), 5.93-6.10 (1H,m), 6.72-7.50 (15H, m)

(5) MASS (m/z): 569 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.48-2.72(1H, m), 2.62 (2/3×3H, s), 2.81 (1/3×3H, s), 2.82-3.05 (2H, m),3.05-3.28 (1H, m), 3.30-3.75 (8H, m), 4.28 (1/3×2H, ABq, Δ=0.15, J=17Hz), 4.33 (2/3×1H, d, J=15 Hz), 4.45-4.63 (1H, m), 4.60 (2/3×1H, d, J=15Hz), 4.98-5.15 (1H, m), 5.92-6.12 (1H, br d), 6.42-7.60 (11H, m)

(6) MASS (m/z): 567 (M+H)⁺ ; NMR (CDCl₃, δ): 1.49 (9H, s), 2.39-2.77(4H, m), 2.58 (3/5×3H, s), 2.80 (2/5×3H, s), 2.90-3.05 (2H, m),3.10-3.40 (2H, m), 3.40-3.80 (8H, m), 4.45-4.60 (1H, m), 4.93-5.10 (1H,m), 5.92-6.08 (1H, m), 6.98-7.48 (11H, m)

(7) MASS (m/z): 611 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45 (9H, s), 2.59 (2/3×3H,s), 2.5-2.6 (1H, m), 2.79 (1/3×3H, s), 3.0-3.1 (2H, m), 3.1-3.2 (1H, m),3.4-3.7 (8H, m), 3.90 (3H, s), 4.33 (1H, d, J=15 Hz), 4.5-4.6 (1H, m),4.69 (1H, d, J=15 Hz), 5.1-5.2 (1H, m), 6.02 (1H, br s), 6.90 (1H, br d,J=9 Hz), 7.0-7.3 (7H, m), 7.8-7.9 (2H, m)

(8) MASS (m/z): 603 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.5-2.6 (1H,m), 2.58 (3/5×3H, s), 2.83 (2/5×3H, s), 3.0-3.1 (2H, m), 3.2-3.3 (1H,m), 3.4-3.7 (8H, m), 4.23 (2/5×1H, d, J=17 Hz), 4.45 (2/5×1H, d, J=17Hz), 4.47 (3/5×1H, d, J=15 Hz), 4.5-4.6 (1H, m), 4.77 (3/5×1H, d, J=15Hz), 5.1-5.3 (1H, m), 6.03 (1H, br d, J=9 Hz), 7.1-7.3 (6H, m), 7.4-7.6(4H, m), 7.7-7.9 (3H, m)

(9) MASS (m/z): 603 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.42-2.62(1H, m), 2.52 (2/3×3H, s), 2.88 (1/3×3H, s), 2.93-3.25 (3H, m),3.35-3.75 (8H, m), 4.40-4.60 (1H, m), 4.65 (1/3×2H, ABq, Δ=0.05, J=17Hz), 4.82 (2/3×1H, d, J=15 Hz), 4.95-5.20 (1H, m), 5.15 (2/3×1H, d, J=15Hz), 6.03 (1H, br d), 6.78-8.05 (13H, m)

(10) MASS (m/z): 554 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.48-2.62(1H, m), 2.70 (2/3×3H, s), 2.85 (1/3×3H, s), 2.95-3.26 (3H, m),3.38-3.75 (8H, m), 4.30 (1/3×2H, ABq, Δ=0.11, J=17 Hz), 4.50-4.60 (1H,m), 4.58 (2/3×2H, ABq, Δ=0.15, J=15 Hz), 5.05-5.20 (1H, m), 5.98 (1H, brd), 6.82-7.63 (9H, m), 8.48 (1H, m)

(11) MASS (m/z): 554 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.48-2.65(1H, m), 2.64 (2/3×3H, s), 2.80 (1/3×3H, s), 2.90-3.28 (3H, m),3.35-3.76 (8H, m), 4.25 (1/3×2H, ABq, Δ=0.12, J=17 Hz), 4.31 (2/3×1H, d,J=15 Hz), 4.50-4.60 (1H, m), 4.59 (2/3×1H, d, J=15 Hz), 4.92-5.22 (1H,m), 6.01 (1H, br d), 6.55-6.90 (2H, m), 7.13-7.48 (6H, m), 8.38-8.51(2H, m)

(12) MASS (FAB) (m/z): 624 (M+H)⁺ ; NMR (CDCl₃, δ): 1.49 (9H, s), 2.30(3H, s), 2.35-2.48 (4H, m), 2.52-2.62 (1H, m), 2.59 (3×2/3H, s), 2.68(3×1/3H, s), 2.94-3.13 (2H, m), 3.20-3.27 (1H, m), 3.42-3.50 (2H, m),3.58-3.65 (2H, m), 3.90 (3H, s), 4.23-4.34 (2×2/3H, m), 4.49-4.58 (1H,m), 4.70 (2×1/3H, d, J=15 Hz), 5.04-5.19 (1H, m), 5.99-6.07 (1H, m),6.88 (2×1/3H, d, J=8 Hz), 7.03 (2×2/3H, d, J=8 Hz), 7.18-7.30 (5H, m),7.37 (1×1/3H, d, J=8 Hz), 7.43 (1×2/3H, d, J=8 Hz), 7.88 (2×1/3H, d, J=8Hz), 7.92 (2×2/3H, d, J=8 Hz)

(13) MASS (FAB) (m/z): 696 (M+H)⁺ ; NMR (CDCl₃, δ): 1.27 (3H, t, J=8Hz), 1.47 (9H, s), 2.52-2.65 (5H, m), 2.62 (3×2/3H, s), 2.78 (3×1/3H,s), 2.92-3.12 (2H, m), 3.14-3.30 (1H, m), 3.26 (2H, s), 3.47-3.54 (2H,m), 3.61-3.70 (2H, m), 3.92 (3H, s), 4.19 (2H, q, J=8 Hz), 4.27-4.32(2×2/3H, m), 4.48-4.58 (1H, m), 4.70 (2×1/3H, d, J=15 Hz), 5.03-5.18(1H, m), 5.95-6.08 (1H, m), 6.88 (2×1/3H, d, J=8 Hz), 7.03 (2×2/3H, d,J=8 Hz), 7.17-7.28 (5H, m), 7.37 (1×1/3H, d, J=8 Hz), 7.44 (1×2/3H, d,J=8 Hz), 7.88 (2×1/3H, d, J=8 Hz), 7.92 (2×2/3H, d, J=8 Hz)

(14) MASS (m/z): 595 (M+); NMR (CDCl₃, δ): 1.48 (9H, s), 2.50 (2/3×3H,s), 2.5-2.6 (2H, m), 2.75 (1/3×3H, s), 2.91 (1/3×6H, s), 2.94 (2/3×6H,s), 3.03 (2H, m), 3.1-3.2 (1H, m), 3.4-3.7 (8H, m), 3.87 (1/3×2H, d,J=16 Hz), 4.24 (1H, d, J=15 Hz), 4.47 (2/3×2H, d, J=15 Hz), 4.5-4.6 (1H,m), 5.0-5.1 (2/3×1H, m), 5.1-5.2 (1/3×1H, m), 6.00 (1H, d, J=9 Hz), 6.60(1/3×2H, d, J=7 Hz), 6.63 (2/3×2H, d, J=7 Hz), 6.80 (1/3×2H, d, J=7 Hz),6.95 (2/3×2H, d, J=7 Hz), 7.1-7.2 (5H, m), 7.45 (1H, d, J=7 Hz)

Preparation 51

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4 or 8.

(1) MASS (m/z): 452 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28 (3H, s), 2.30-2.65(5H, m), 2.81 (2/3×3H, s), 2.85-2.98 (1H, m), 2.89 (1/3×3H, s),3.30-3.88 (5H, m), 4.44 (1/3×2H, ABq, Δ=0.22, J=17 Hz), 4.60 (2/3×2H,ABq, Δ=0.14, J=15 Hz), 5.78-5.92 (1H, m), 6.90-7.47 (10H, m), 8.60-8.78(1H, m)

(2) MASS (m/z): 509 (M+H)⁺ ; NMR (CDCl₃, δ): 2.20-2.48 (5H, m), 2.31(3H, s), 2.63 (3/5×3H, s), 2.70-2.88 (1H, m), 2.82 (2/5×3H, s),2.90-3.15 (2H, m), 2.92 (2/5×6H, s), 2.94 (3/5×6H, s), 3.35-3.76 (5H,m), 4.23 (2/5×2H, ABq, Δ=0.21, J=17 Hz), 4.28 (3/5×1H, d, J=15 Hz), 4.54(3/5×1H, d, J=15 Hz), 5.06-5.32 (1H, m), 6.45-7.33 (9H, m), 8.02-8.20(1H, m)

(3) MASS (m/z): 523 (M+H)⁺ ; NMR (CDCl₃, δ): 2.22 (2/5×6H, s), 2.24(3/5×6H, s), 2.25-2.52 (5H, m), 2.30 (3H, s), 2.66(3/5×3H, s), 2.70-2.90(1H, m), 2.88 (2/5×3H, s), 2.90-3.18 (2H, m), 3.33-3.75 (7H, m), 4.32(3/5×1H, d, J=15 Hz), 4.33 (2/5×2H, s), 4.66 (3/5×1H, d, J=15 Hz),5.10-5.23 (1H, m), 6.90-7.32 (9H, m), 8.02-8.20 (1H, m)

(4) MASS (m/z): 478 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.87(7H, m), 2.95-3.30 (3H, m), 3.38-3.85 (7H, m), 4.04 (1/2×1H, d, J=17Hz), 4.53 (1/2×1H, d, J=17 Hz), 4.67 (1/2×2H, ABq, Δ=0.17, J=17 Hz),5.14-5.28 (1H, m), 6.82-7.25 (9H, m), 8.10-8.22 (1H, m)

(5) MASS (m/z): 500 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.57(5H, m), 2.68 (3/4×3H, s), 2.70-2.88 (1H, m), 2.82 (1/4×3H, s),2.90-3.18 (2H, m), 3.35-3.75 (5H, m), 4.25 (3/4×1H, d, J=15 Hz), 4.30(1/4×2H, ABq, Δ=0.05, J=17 Hz), 4.64 (3/4×1H, d, J=15 Hz), 5.05-5.22(1H, m), 6.80-7.01 (2H, m), 7.10-7.30 (7H, m), 8.05-8.20 (1H, m)

(6) MASS (m/z): 544, 546 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s),2.30-2.57 (5H, m), 2.67 (3/4×3H, s), 2.70-2.88 (1H, m), 2.82 (1/4×3H,s), 2.90-3.18 (2H, m), 3.35-3.75 (5H, m), 4.23 (3/4×1H, d, J=15 Hz),4.29 (1/4×2H, ABq, Δ=0.06, J=17 Hz), 4.62 (3/4×1H, d, J=15 Hz),5.05-5.21 (1H, m), 6.74-6.95 (2H, m), 7.11-7.42 (7H, m), 8.05-8.20 (1H,m)

(7) MASS (m/z): 484 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.3-2.55 (5H,m), 2.68 (3/4×3H, s), 2.72-2.88 (1H, m), 2.83 (1/4×3H, s), 2.90-3.18(2H, m), 3.35-3.75 (5H, m), 4.27 (3/4×1H, d, J=15 Hz), 4.30 (1/4×2H, s),4.62 (3/4×1H, d, J=15 Hz), 5.10-5.22 (1H, m), 6.83-7.08 (4H, m),7.13-7.32 (5H, m), 8.05-8.20 (1H, m)

(8) MASS (m/z): 497 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.55(4H, m), 2.65 (3/4×3H, s), 2.75-2.88 (1H, m), 2.78 (1/4×3H, s),2.93-3.15 (2H, m), 3.35-3.75 (6H, m), 3.90 (1/4×3H, s), 3.92 (3/4×3H,s), 4.20 (1/4×2H, ABq, Δ=0.18, J=17 Hz), 4.24 (3/4×1H, d, J=15 Hz), 4.55(3/4×1H, d, J=15 Hz), 5.05-5.25 (1H, m), 6.58-6.70 (1H, m), 7.02-7.35(6H, m), 7.80-8.20 (2H, m)

(9) MASS (m/z): 480 (M+H)⁺ ; NMR (CDCl₃, δ): 0.99 (3/5×3H, t, J=7 Hz),1.04 (2/5×3H, t, J=7 Hz), 2.20-2.50 (5H, m), 2.28 (3H, s), 2.68-2.88(1H, m), 2.90-3.30 (4H, m), 3.32-3.75 (5H, m), 4.23 (3/5×1H, d, J=15Hz), 4.33 (2/5×2H, ABq, Δ=0.05, J=17 Hz), 4.83 (3/5×1H, d, J=15 Hz),5.00-5.22 (1H, m), 6.92-7.40 (10H, m), 8.00-8.20 (1H, m)

(10) MASS (m/z): 501 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30-2.60 (5H, m), 2.31(3H, s), 2.68 (4/5×3H, s), 2.72-2.88 (1H, m), 2.78 (1/5×3H, s),2.92-3.24 (2H, m), 3.37-3.75 (5H, m), 4.28 (4/5×1H, d, J=15 Hz), 4.29(1/5×2H, s), 4.60 (4/5×1H, d, J=15 Hz), 5.05-5.20 (1H, m), 7.00-7.37(9H, m), 8.02-8.22 (2H, m)

(11) MASS (m/z): 481 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s), 2.31-2.50(5H, m), 2.51 (1/4×3H, s), 2.54 (3/4×3H, s), 2.66 (3/4×3H, s), 2.72-2.88(1H, m), 2.80 (1/4×3H, s), 2.93-3.20 (2H, m), 3.38-3.76 (5H, m), 4.28(1/4×2H, ABq, Δ=0.14, J=17 Hz), 4.31 (3/4×1H, d, J=15 Hz), 4.59 (3/4×1H,d, J=15 Hz), 5.06-5.24 (1H, m), 6.98-7.32 (7H, m), 8.08-8.33 (2H, m)

(12) MASS (m/z): 468 (M+H)⁺ ; NMR (CDCl₃, δ): 2.38-2.59 (1H, m), 2.51(1/4×3H, s), 2.53 (3/4×3H, s), 2.65 (3/4×3H, s), 2.69-2.86 (1H, m), 2.79(1/4×3H, s), 2.92-3.18 (2H, m), 3.32-3.76 (9H, m), 4.27 (1/4×2H, ABq,Δ=0.16, J=17 Hz), 4.32 (3/4×1H, d, J=15 Hz), 4.57 (3/4×1H, d, J=15 Hz),5.03-5.22 (1H, m), 6.98-7.33 (7H, m), 8.05-8.34 (2H, m)

(13) MASS (m/z): 533 (M+H)⁺ ; NMR (CDCl₃, δ): 2.27-2.58 (5H, m), 2.30(3H, s), 2.70-2.88 (1H, m), 2.72 (2/3×3H, s), 2.85 (1/3×3H, s),2.92-3.21 (2H, m), 3.33-3.78 (5H, m), 4.38 (1/3×2H, s), 4.41 (2/3×1H, d,J=15 Hz), 4.67 (2/3×1H, d, J=15 Hz), 5.08-5.24 (1H, m), 7.00-7.36 (7H,m), 7.50-7.64 (2H, m), 8.10 (1H, s), 8.10-8.22 (1H, m), 8.52 (1H, s)

(14) MASS (m/z): 501 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s), 2.31-2.62(5H, m), 2.68 (4/5×3H, s), 2.71-2.88 (1H, m), 2.82 (1/5×3H, s),2.95-3.20 (2H, m), 3.35-3.78 (5H, m), 4.30 (4/5×1H, d, J=15 Hz), 4.32(1/5×2H, ABq, Δ=0.05, J=17 Hz), 4.62 (4/5×1H, d, J=15 Hz), 5.03-5.20(1H, m), 7.10-7.32 (5H, m), 7.48 (1H, s), 8.08-8.31 (2H, m), 8.40-8.52(1H, m)

(15) MASS (m/z): 488 (M+H)⁺ ;

NMR (CDCl₃, δ): 2.33-2.62 (1H, m), 2.68 (4/5×3H, s), 2.71-2.85 (1H, m),2.79 (1/5×3H, s), 2.90-3.22 (2H, m), 3.34-3.77 (9H, m), 4.28 (1/5×2H,ABq, Δ=0.05, J=17 Hz), 4.29 (4/5×1H, d, J=15 Hz), 4.58 (4/5×1H, d, J=15Hz), 5.02-5.18 (1H, m), 7.00-7.38 (7H, m), 8.00-8.21 (2H, m)

(16) MASS (m/z): 454 (M+H)⁺ ; NMR (CDCl₃, δ): 2.38-2.61 (1H, m), 2.67(3/4×3H, s), 2.67-2.85 (1H, m), 2.82 (1/4×3H, m), 2.92-3.20 (2H, m),3.35-3.76 (9H, m), 4.32 (1/4×2H, ABq, Δ=0.10, J=17 Hz), 4.32 (3/4×1H, d,J=15 Hz), 4.64 (3/4×1H, d, J=15 Hz), 5.07-5.21 (1H, m), 7.05-7.43 (7H,m), 8.06-8.22 (7H, m), 8.29(1/4×1H, s), 8.40 (3/4×1H, s), 8.46-8.56 (1H,m)

(17) MASS (m/z): 467 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s), 2.31-2.58(5H, m) 2.67 (3/4×3H, s), 2.70-2.86 (1H, m), 2.82 (1/4×3H, s), 2.94-3.20(2H, m), 3.38-3.75 (5H, m), 4.32 (3/4×1H, d, J=5 Hz), 4.34 (1/4×2H, ABq,Δ=0.06, J=17 Hz), 4.65 (3/4×1H, d, J=15 Hz), 5.08-5.20 (1H, m),7.11-7.42 (7H, m), 8.07-8.22 (1H, m), 8.28 (1/4×1H, s), 8.41 (3/4×1H,s), 8.48-8.56 (1H, m)

(18) MASS (m/z): 480 (M+H)⁺ ; NMR (CDCl₃, δ): 1.09 (3H, t, J=7 Hz),2.22-2.52 (7H, m), 2.67 (2/3×3H, s), 2.69-2.92 (1H, m), 2.87 (1/3×3H,s), 2.92-3.15 (2H, m), 3.34-3.78 (5H, m), 4.33 (2/3×1H, d, J=15 Hz),4.38 (1/3×2H, ABq, Δ=0.07, J=17 Hz), 4.68 (2/3×1H, d, J=15 Hz),5.09-5.23 (1H, m), 6.92-7.32 (10H, m), 8.02-8.22 (1H, m)

(19) NMR (CDCl₃, δ): 2.30 (3H, s), 2.37 (4H, m), 2.44 (1H, dd, J=7, 16Hz), 2.65 (3H×2/3, s), 2.72-2.85 (1H, m), 2.83 (3H×1/3, s), 2.94-3.12(2H, m), 3.43 (2H, m), 3.57-3.74 (3H, m), 3.79 (3H, s), 4.20 (1H×1/3, d,J=15 Hz), 4.26 (1H×2/3, d, J=15 Hz), 4.33 (1H×1/3, d, J=15 Hz), 4.61(1H×2/3, d, J=15 Hz), 5.11-5.24 (1H, m), 6.77-7.28 (9H, m), 8.08(1H×1/3, d, J=8 Hz), 8.15 (1H×2/3, d, J=8 Hz)

(20) MASS (ESI) (m/z): 480 (M+H); NMR (CDCl₃, δ): 2.29 (3H, s), 2.30(3H, s), 2.23-2.48 (6H, m), 2.63 (3×2/3H, s), 2.70-2.80 (1H, m), 2.84(3×1/3H, s), 2.89-3.13 (2H, m), 3.38-3.47 (2H, m), 3.50-3.72 (2H, m),4.23-4.31 (2×2/3H, m), 4.62 (2×1/3H, d, J=15 Hz), 5.10-5.22 (1H, m),6.87 (2×1/3H, d, J=8 Hz), 6.94 (2×2/3H, d, J=8 Hz), 7.07 (2H, d, J=8Hz), 7.12-7.29 (5H, m), 8.08 (1×1/3H, d, J=8 Hz), 8.15 (1×2/3H, d, J=8Hz)

(21) NMR (CDCl₃, δ): 2.29 (3H, s), 2.36 (4H, m), 2.66-2.77 (1H, m),2.87-3.09 (1H, m), 2.95 (3H×1/3, s), 3.02 (3H×2/3, s), 3.42-3.69 (5H,m), 3.76-3.93 (3H, m), 4.57 (1H×2/3, d, J=15 Hz), 4.66 (2H×1/3, s), 4.67(1H×2/3, d, J=15 Hz), 5.03 (1H, m), 7.16-7.36 (5H, m), 8.42 (1H×1/3, d,J=8 Hz), 8.50 (1H×2/3, d, J=8 Hz)

(22) NMR (CDCl₃, δ): 0.81 (3H×1/3, d, J=7 Hz), 0.84 (3H×1/3, d, J=7 Hz),0.94 (3H×2/3, d, J=7 Hz), 0.98 (3H×2/3, d, J=7 Hz), 1.42-1.72 (3H, m),2.29 (3H, s), 2.33-2.42 (4H, m), 2.51-2.62 (1H, m), 2.86-2.97 (1H, m),2.93 (3H×1/3, s), 3.01 (3H×2/3, s), 3.46-3.77 (5H, m), 4.43 (1H×2/3, d,J=15 Hz), 4.61 (1H×1/3, d, J=16 Hz), 4.73 (1H×1/3, d, J=16 Hz), 4.74(1H×2/3, d, J=15 Hz), 4.98 (1H, dt, J=4, 8 Hz), 7.18-7.37 (5H, m), 7.97(1H×1/3, d, J=8 Hz), 8.04 (1H×2/3, d, J=8 Hz)

(23) NMR (CDCl₃, δ): 2.30 (3H, s), 2.35-2.44 (4H, m), 2.52 (1H, dd, J=8,16 Hz), 2.71 (3H×2/3, s), 2.77 (1H, dd, J=3, 16 Hz), 2.85 (3H×1/3, s),2.93-3.17 (2H, m), 3.41-3.47 (2H, m), 3.54-3.74 (3H, m), 4.35 (1H×1/3,d, J=15 Hz), 4.37 (1H×2/3, d, J=15 Hz), 4.50 (1H×1/3, d, J=15 Hz), 4.72(1H×2/3, d, J=15 Hz), 5.07 (1H×1/3, q, J=7 Hz), 5.18 (1H×2/3, q, J=7Hz), 7.01 (1H×2/3, d, J=8 Hz), 7.13 (2H, d, J=8 Hz), 7.20-7.25 (3×1/3H,m), 7.50 (2H, t, J=8 Hz)

(24) NMR (CDCl₃, δ): 2.30 (3H, s), 2.36 (4H, m), 2.50 (1H, dd, J=7, 16Hz), 2.67 (3H×3/5, s), 2.81 (1H×2/5, dd, J=4, 16 Hz), 2.88 (3H×2/5, s),2.90 (1H×3/5, dd, J=4, 16 Hz), 2.97-3.12 (2H, m), 3.39-3.46 (2H, m),3.56-3.77 (3H, m), 4.32 (1H×3/5, d, J=15 Hz), 4.32 (1H×2/5, d, J=15 Hz),4.44 (1H×2/5, d, J=15 Hz), 4.70 (1H×3/5, d, J=15 Hz), 5.15 (1H, m),7.00-7.28 (10H, m), 8.02 (1H×2/5, d, J=8 Hz), 8.13 (1H×3/5, d, J=8 Hz)

(25) NMR (CDCl₃, δ): 2.29 (3H, s), 2.25-2.50 (5H, m), 2.66 (3H×2/3, s),2.73 (1H×1/3, dd, J=3, 16 Hz), 2.82 (1H×2/3, dd, J=3, 16 Hz), 2.87(3H×1/3, s), 2.92-3.13 (2H, m), 3.38-3.47 (2H, m), 3.54-3.73 (3H, m),4.33 (1H×2/3, d, J=15 Hz), 4.34 (1H×1/3, d, J=15 Hz), 4.41 (1H×1/3, d,J=15 Hz), 4.67 (1H×2/3, d, J=15 Hz), 5.17 (1H, m), 6.97-7.15 (3H, m),7.21 (3H, s), 7.22-7.27 (4H, m), 8.06 (1H×1/3, d, J=7 Hz), 8.16 (1H×2/3,d, J=7 Hz)

(26) NMR (CDCl₃, δ): 2.30 (3H, s), 2.36 (4H, m), 2.50 (1H, dd, J=7, 16Hz), 2.67 (3H×3/5, s), 2.81 (1H×2/5, dd, J=4, 16 Hz), 2.88 (3H×2/5, s),2.90 (1H×3/5, dd, J=4, 16 Hz), 2.97-3.12 (2H, m), 3.39-3.46 (2H, m),3.56-3.77 (3H, m), 4.32 (1H×3/5, J=15 Hz), 4.32 (1H×2/5, J=15 Hz), 4.44(1H×2/5, J=15 Hz), 4.70 (1H×3/5, J=15 Hz), 5.15 (1H, m), 7.00-7.28 (10H,m), 8.02 (1H×2/5, d, J=8 Hz), 8.13 (1H×3/5, d, J=8 Hz)

(27) MASS (FAB) (m/z): 538 (M+H)⁺ ; NMR (CDCl₃, δ): 1.28 (3H, t, J=8Hz), 2.25-2.33 (1×1/3H, m), 2.41-2.49 (1×2/3H, m), 2.51-2.62 (4H, m),2.63 (3×2/3H, s), 2.70-2.85 (1H, m), 2.86 (3×1/3H, s), 2.92-3.13 (2H,m), 3.23 (2H, s), 3.42-3.51 (2H, m), 3.57-3.77 (3H, m), 4.19 (2H, q, J=8Hz), 4.31-4.42 (2×2/3H, m), 4.68 (2×1/3H, d, J=15 Hz), 5.11-5.20 (1H,m), 6.98 (2×1/3H, d, J=8 Hz), 7.05 (2×2/3H, d, J=8 Hz), 7.12-7.31 (8H,m), 8.07 (1×1/3H, d, J=8 Hz), 8.15 (1×2/3H, d, J=8 Hz)

(28) MASS: 524 (M+1); NMR (CDCl₃, δ): 2.29 (3H, s), 2.33-2.45 (4H, m),2.48-2.57 (1H, m), 2.63 (3×2/3H, s), 2.71-2.81 (1H, m), 2.83 (3×1/3H,s), 2.92-3.14 (2H, m), 3.39-3.47 (2H, m), 3.52-3.73 (3H, m), 3.88 (3H,s), 4.33-4.49 (2×2/3H, m), 4.72 (2×1/3H, d, J=15 Hz), 5.07-5.22 (1H, m),6.98 (2×1/3H, d, J=8 Hz), 7.08 (2×2/3H, d, J=8 Hz), 7.13-7.30 (5H, m),7.92 (2H, t, J=8 Hz), 8.10 (1×1/3H, d, J=8Hz), 8.17 (1×2/3H, d, J=8 Hz)

(29) MASS (FAB) (m/z): 596 (M+H)⁺ ; NMR (CDCl₃, δ): 1.22 (3H, t, J=8Hz), 2.33-2.42 (1H, m), 2.48-2.62 (4H, m), 2.63 (3×2/3H, s), 2.69-2.78(1H, m), 2.80 (3×1/3H, s), 2.92-3.13 (2H, m), 3.20 (2H, s), 3.42-3.51(2H, m), 3.57-3.72 (3H, m), 3.90 (3H, s), 4.19 (2H, q, J=8 Hz),4.31-4.50 (2×2/3H, m), 4.72 (2×1/3H, d, J=15 Hz), 5.07-5.12 (1H, m),6.98 (2×1/3H, d, J=8 Hz), 7.08 (2×2/3H, d, J=8 Hz), 7.12-7.17 (1H, m),7.20-7.28 (4H, m), 7.92 (2H, t, J=8 Hz), 8.10 (1×1/3H, d, J=8 Hz), 8.17(1×2/3H, d, J=8 Hz)

Preparation 52

To a solution of Starting compound (53.06 g) in dichloromethane (400 ml)were added N-methyl-N-(3-pyridylmethyl)amine (25.65 g) and1-hydroxybenzotriazole (27.02 g) and the mixture was cooled with ice.1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (42.18 g)was added to the mixture in small portions, then the whole was stirredat room temperature for 8 hours. After the mixture was concentrated, 1Nsodium hydroxide (300 ml) was added thereto, and the mixture wasextracted three times with ethyl acetate. The organic layer was washedonce with brine and dried over magnesium sulfate. Evaporation of thesolvent followed by silica gel column chromatography(chloroform-methanol) gave Object compound (81.37 g) as a colorless oil.

MASS: m/z 370 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (1/5×9H, s), 1.42 (4/5×3H,s), 2.63 (4/5×3H, s), 2.79 (1/5×3H, s), 2.92-3.06 (2H, m), 4.08 (1/5×1H,d, J=17 Hz), 4.35 (1/5×1H, d, J=17 Hz), 4.49 (4/5×2H, ABq, Δ=0.09, J=15Hz), 4.79-4.98 (1H, m), 5.28-5.42 (1H, m), 7.10-7.35 (7H, m), 8.28(1/5×1H, s), 8.42 (4/5×1H, s), 8.50-8.55 (1H, m)

Preparation 53

Object compounds were obtained according to a similar manner to that ofPreparation 1, 6, 11 or 52.

(1) MASS: m/z 404 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.63 (5/6×3H,s), 2.76 (1/6×3H, s), 2.88-3.09 (2H, m), 4.04 (1/6×1H, d, J=17 Hz), 4.30(1/6×1H, d, J=17 Hz), 4.44 (5/6×2H, ABq, Δ=0.08, J=15 Hz), 4.76-4.92(1H, m), 5.22-5.38 (1H, m), 7.03-7.40 (7H, m), 8.05 (1/6×1H, d, J=2 Hz),8.18 (5/6×1H, d, J=2 Hz)

(2) MASS: m/z 370 (M+H)⁺ ; NMR (CDCl₃, δ): 1.39 (1/4×9H, s), 1.42(3/4×9H, s), 2.69 (3/4×3H, s), 2.82 (1/4×3H, s), 2.90-3.12 (2H, m), 4.28(1/4×2H, s), 4.48 (3/4×2H, ABq, Δ=0.06, J=15 Hz), 4.68-4.98 (1H, m),5.20-5.40 (1H, m), 6.73-7.35 (7H, m), 8.40-8.52 (2H, m)

Preparation 54

Trifluoroacetic acid (150 ml) was slowly added to ice-cooled Startingcompound (72.82 g), and the mixture was stirred at room temperature for2.5 hours. The trifluoroacetic acid was evaporated and the residue wascooled with ice. 1510 Aqueous sodium hydroxide (about 400 ml) was addedto the residue, and the mixture was extracted three times withchloroform. The organic layer was dried over magnesium sulfate.Evaporation of the solvent gave Object compound (62.01 g) as a colorlessoil.

MASS: m/z 270 (M+H)⁺ ; NMR (CDCl₃, δ): 2.71 (3/4×3H, s), 2.76-3.10 (2H,m), 2.88 (1/4×3H, s), 3.82-4.02 (1H, m), 4.28 (1/4×2H, ABq, Δ=0.20, J=17Hz), 4.55 (3/4×2H, ABq, Δ=0.21, J=15 Hz), 7.11-7.55 (7H, m), 8.32-8.58(2H, m)

Preparation 55

Object compound was obtained according to a similar manner to that ofPreparation 3, 4, 8, 41 or 54.

MASS: m/z 303 (M+H)⁺ ; NMR (CDCl₃, δ): 2.49 (5/6×3H, s), 2.72 (1/6×3H,s), 2.98-3.23 (2H, m), 3.70 (1/6×1H, d, J=17 Hz), 4.23 (1/6×1H, d, J=17Hz), 4.40 (1H, t, J=7 Hz), 4.42 (5/6×2H, ABq, Δ=0.07, J=15 Hz),7.08-7.52 (7H, m), 8.06 (1/6×1H, d, J=2 Hz), 8.20 (5/6×1H, d, J=2 Hz)

Preparation 56

To a stirred solution of(2S)-3-(2-pyridyl)-2-(tert-butoxycarbonylamino)propionic acid (1.19 g)and Starting Compound (1.20 g) in N,N-dimethylformamide (3 ml) was addeddropwise diphenylphosphoryl azide (1.25 g) followed by triethylamine(1.36 ml) at 0° C. The mixture was stirred at room temperature for 3hours. The reaction mixture was diluted with water and extracted withchloroform. The extract was dried and evaporated. The residue waspurified by column chromatography on silica gel in chloroform ˜2%methanol-chloroform. Recrystallization from ethyl acetate--n-hexane gaveObject Compound (1.69 g).

MASS: m/z 518 (M⁺ +1); NMR (CDCl₃, δ): 1.44 (9H, s), 2.52 (3H×3/4, s),2.74 (3H×1/4, s), 2.80 (2H×3/4, d, J=7 Hz), 2.93 (2H×1/4, m), 3.19 (1H,m), 3.35 (1H, m), 4.08 (1H×1/4, d, J=16 Hz), 4.21 (1H×1/4, d, J=16 Hz),4.27 (1H×3/4, d, J=15 Hz), 4.56 (1H×3/4, d, J=15 Hz), 4.57 (1H, m), 5.06(1H, q, J=7 Hz), 6.43 (1H, m), 7.05-7.35 (9H, m), 7.60 (2H, m), 8.21(1H×1/4, d, J=2 Hz), 8.35 (1H×3/4, d, J=2 Hz), 8.51 (2H, m)

Preparation 57

Object compounds were obtained according to a similar manners to that ofPreparation 1, 6, 11, 38, 52 or 56.

(1) MASS: m/z 555 (M⁺ +1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.47 (3H×2/3,s), 2.75 (3H×1/3, s), 2.85 (2H, m), 3.12-3.32 (2H, m), 4.11 (1H×1/3, d,J=16 Hz), 4.18 (1H×1/3, d, J=16 Hz), 4.22 (1H×2/3, d, J=15 Hz), 4.52(1H×2/3, d, J=15 Hz), 5.02 (1H, m), 5.13 (1H, m), 6.68 (1H, t, J=8 Hz),6.87-7.35 (15H, m), 7.62 (1H, m), 8.13 (1H×2/3, s), 8.16 (1H×1/3, s)

(2) MASS: m/z 506 (M⁺ +1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.63 (3H×2/3,s), 2.83 (3H×1/3, s), 2.91-3.02 (3H, m), 3.12 (1H, m), 4.16 (1H×1/3, d,J=16 Hz), 4.34-4.54 (2×2/3H, m), 5.05 (1H, m), 6.81 (1H, s), 6.99-7.13(4H, m), 7.21-7.28 (7H, m), 7.47 (1H, d, J=8 Hz)

(3) MASS: m/z 552 (M⁺); NMR (CDCl₃, δ): 1.44 (9H, s), 2.53 (3H×2/3, s),2.71 (3H×1/3, s), 2.79 (2H, d, J=8 Hz), 3.19 (1H, m), 3.33 (1H, m), 4.23(1H×2/3, d, J=15 Hz), 4.26 (1H×1/3, d, J=16 Hz), 4.48 (1H×1/3, d, J=16Hz), 4.51 (1H×2/3, d, J=15 Hz), 4.57 (1H, m), 5.05 (1H, m), 6.43 (1H,m), 7.06-7.25 (10H, m), 7.60 (1H, m), 8.12 (1H, m), 8.51 (1H, m)

(4) MASS: m/z 518 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.62 (3H×3/4,s), 2.77 (3H×1/4, s), 2.82-2.98 (2H, m), 3.12-3.33 (2H, m), 4.02-4.54(3H, m), 4.93 (1H×1/4, m), 5.12 (1H×3/4, m), 6.63-6.68 (2H×1/4, m),6.82-6.84 (2H×3/4, m), 7.06-7.24 (7H, m), 7.54-7.62 (2H, m), 8.37-8.52(3H, m)

(5) MASS: m/z 517 (M⁺ +1); NMR (CDCl₃, δ): 1.44 (9H, s), 2.49 (3H×3/4,s), 2.76 (3H×1/4, s), 2.72-2.95 (2H, m), 3.08-3.37 (2H, m), 4.17(1H×1/4, d, J=15 Hz), 4.30 (1H×3/4, d, J=15 Hz), 4.34 (1H×1/4, d, J=15Hz), 4.53 (1H×3/4, d, J=15 Hz), 4.57 (1H, m), 5.08 (1H, m), 6.84-7.26(13H, m), 7.53-7.62 (2H, m), 8.49-8.52 (1H, m)

Preparation 58

Object compounds were obtained according to a similar manner to that ofPreparation 3, 4, 8, 41 or 54.

(1) NMR (CDCl₃, δ): 2.77 (3H×3/4, s), 2.86 (3H×1/4, s), 2.87-3.08 (3H,m), 3.17-3.35 (1H, m), 3.74-3.85 (1H, m), 4.32 (1H×3/4, d, J=15 Hz),4.37 (1H×1/4, d, J=15 Hz), 4.58 (1H×1/4, d, J=15 Hz), 4.62 (1H×3/4, d,J=15 Hz), 4.97-5.06 (1H×1/4, m), 5.15-5.25 (1H×3/4, m), 6.75-6.79(2H×1/4, m), 6.87-6.89 (2H×3/4, m), 7.14-7.27 (7H, m), 7.56-7.64 (1H,m), 8.08-8.23 (1H, m), 8.44-8.52 (3H, m)

(2) NMR (CDCl₃, δ): 2.67 (3H×2/3, s), 2.85 (3H×1/3, s), 2.88-3.07 (3H,m), 3.17-3.31 (1H, m), 3.72-3.87 (1H, m), 4.32 (1H×2/3, d, J=15 Hz),4.33 (1H×1/3, d, J=15 Hz), 4.63 (1H×1/3, d, J=15 Hz), 4.65 (1H×2/3, d,J=15 Hz), 6.96-7.29 (12H, m), 7.55-7.63 (1H, m), 8.17-8.28 (1H, m),8.48-8.52 (1H, m)

(3) NMR (CDCl₃, δ): 2.67 (3H×2/3, s), 2.75 (3H×1/3, s), 2.92 (3H, m),3.18-3.31 (1H, m), 3.74 (1H, m), 4.23 (1H×1/3, d, J=16 Hz), 4.25(1H×2/3, d, J=15 Hz), 4.53 (1H×1/3, d, J=16 Hz), 4.56 (1H×2/3, d, J=15Hz), 7.10-7.30 (10H, m), 7.56 (1H, m), 8.00-8.20 (2H, m), 8.49 (1H, m)

(4) NMR (CDCl₃, δ): 2.72 (3H×2/3, s), 2.79-3.06 (4H, m), 2.87 (3H×1/3,s), 3.49 (1H×1/3, dd, J=4, 7 Hz), 3.58 (1H×2/3, t, J=6 Hz), 4.32(1H×1/3, d, J=16 Hz), 4.37 (1H×2/3, d, J=15 Hz), 4.44 (1H×1/3, d, J=16Hz), 4.65 (1H×2/3, d, J=15 Hz), 5.15 (1H, q, J=7 Hz), 6.78 (1H, d, J=10Hz), 7.01-7.28 (10H, m), 7.47 (1H, d, J=2 Hz), 8.03 (1H×1/3, d, J=8 Hz),8.07 (1H×2/3, d, J=8 Hz)

(5) NMR (CDCl₃, δ): 2.71 (3H×2/3, s), 2.86 (3H×1/3, s), 2.85-3.04 (3H,m), 3.23 (1H×1/3, dd, J=3, 15 Hz), 3.30 (1H×2/3, dd, J=3, 15 Hz), 3.61(1H×1/3, dd, J=4, 15 Hz), 3.69 (1H×2/3, dd, J=4, 15 Hz), 4.29 (1H×2/3,d, J=15 Hz), 4.41 (2H×1/3, s), 4.68 (1H×2/3, d, J=15 Hz), 5.21 (1H, m),6.96-7.37 (14H, m), 7.67 (1H, m), 7.94-8.16 (2H, m)

(6) NMR (CDCl₃, δ): 2.69 (3H×3/4, s), 2.82 (3H×1/4, s), 2.85-3.03 (3H,m), 3.18-3.30 (1H, m), 3.69 (1H×1/4, dd, J=3, 7 Hz), 3.77 (1H×3/4, dd,J=3, 7 Hz), 4.30 (1H×1/4, d, J=16 Hz), 4.32 (1H×3/4, d, J=15 Hz), 4.38(1H×1/4, d, J=16 Hz), 4.65 (1H×3/4, d, J=15 Hz), 5.15 (1H, m), 7.14-7.27(8H, m), 7.37 (1H, m), 7.61 (1H, m), 8.21-8.53 (4H, m)

Preparation 59

The following object compound was obtained according to a similar mannerto that of Preparation 1, 6, 11, 38, 52 or 58.

MASS: 486 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.09 (3×1/3H, s), 2.11(3×2/3H, s), 2.57 (3×2/3H, s), 2.82 (3×1/3H, s), 2.79-2.88 (2H, m),2.99-3.04 (2H, m), 4.08 (2×1/6H, d, J=16 Hz), 4.31 (2×1/6H, d, J=16 Hz),4.39 (2×1/3H, d, J=15 Hz), 4.59 (2×1/3H, d, J=15 Hz), 4.20-4.32 (1H, m),5.11-5.20 (1H, m), 5.22-5.37 (1H, m), 6.93-7.32 (11H, m)

Preparation 60

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS: 491 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.69 (3×4/5H, s),2.77 (3×1/5H, s), 2.92-3.13 (2H, m), 3.35 (1H, t, J=8 Hz), 3.57-3.63(1H, m), 3.90-4.03 (1H, m), 4.12-4.25 (1H, m), 4.35 (2×1/10H, d, J=16Hz), 4.40 (2×1/10H, d, J=16 Hz), 4.39 (2×2/5H, d, J=15 Hz), 4.50(2×2/5H, d, J=15 Hz), 5.10 (1H, q, J=8 Hz), 5.43 (1H, d, J=8 Hz),7.09-7.19 (2H, m), 7.20-7.32 (5H, m), 7.39 (1H, d, J=8 Hz), 8.10(1×1/5H, s), 8.19 (1×4/5H, s)

(2) MASS: 714 (M+1); NMR (CDCl₃, δ): 1.42 (9H, s), 1.48-1.53 (1H, m),1.54 (3×2/3H, s), 2.64-2.73 (1H, m), 2.77 (3×1/3H, s), 2.89-3.03 (2H,m), 3.85-3.95 (1H, m), 4.17-4.34 (2×2/3H, m), 4.54 (2×1/3H, d, J=15 Hz),4.67-4.77 (1H, m), 5.04-5.13 (1H, m), 6.72-7.31 (20H, m), 7.39-7.43 (6H,m)

(3) MASS: 507 (M+1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.73 (3×3/4H, s),2.88 (3×1/4H, s), 2.93-3.12 (2H, m), 3.24-3.33 (1H, m), 3.52-3.64 (1H,m), 3.92-4.08 (1H, m), 4.13-4.24 (1H, m), 4.60 (2×1/2H, d, J=15 Hz),4.78 (2×1/2H, d, J=15 Hz), 5.10-5.20 (1H, m), 5.38-5.47 (1H, m),7.10-7.20 (6H, m), 7.58 (1H, t, J=8 Hz), 7.71 (1H, t; J=8 Hz), 7.80 (1H,d, J=8 Hz), 7.82 (1×1/4H, s), 7.92 (1×3/4H, s), 8.10 (1H, dd, J=8, 2Hz), 8.70 (1×1/4H, d, J=2 Hz), 8.76 (1×3/4H, d, J=2 Hz)

(4) MASS (m/z): 516 (M⁺ +1); NMR (CDCl₃, δ): 2.52 (3H×2/3, s), 2.79(3H×1/3, s), 2.97 (2H, m), 3.04 (2H, m), 4.02 (1H×1/3, d, J=15 Hz), 4.25(1H×1/3, d, J=15 Hz), 4.34 (1H×2/3, d, J=15 Hz), 4.37 (1H, m), 4.54(1H×2/3, d, J=15 Hz), 4.92 (1H, m), 5.11 (1H, m), 6.68 (1H×1/3, d, J=8Hz), 6.79 (1H×2/3, d, J=8 Hz), 6.91 (1H, m), 7.04-7.30 (14H, m)

(5) MASS (m/z): 457 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.75 (3H×3/4,s), 2.86 (3H×1/4, s), 2.91-3.12 (2H, m), 3.57-3.65 (1H, m), 3.97 (1H,m), 4.20 (1H, m), 4.28 (1H×1/4, d, J=15 Hz), 4.33 (1H×1/4, d, J=15 Hz),4.44 (1H×3/4, d, J=15 Hz), 4.54 (1H×3/4, d, J=15 Hz), 4.98-5.07 (1H×1/4,m), 5.13-5.21 (1H×3/4, m), 5.46 (1H, t, J=7 Hz), 6.88 (1H×1/4, d, J=7Hz), 6.94 (1H×3/4, d, J=7 Hz), 7.10-7.28 (5H, m), 8.49 (2H, d, J=7 Hz)

(6) MASS (m/z): 457 (M⁺ +1); NMR (CDC₃, δ): 1.46 (9H, s), 2.70 (3H×3/4,s), 2.82 (3H×1/4, s), 3.02 (2H, m), 3.38 (1H, m), 3.61 (1H, m), 3.97(1H, m), 4.07 (1H×1/4, d, J=15 Hz), 4.21 (1H, m), 4.42 (1H×1/4, d, J=15Hz), 4.44 (1H×3/4, d, J=15 Hz), 4.57 (1H×3/4, d, J=15 Hz), 5.12 (1H, m),5.44 (1H, m), 7.13-7.29 (7H, m), 7.44 (1H, m), 8.34 (1H×1/4, d, J=2 Hz),8.42 (1H×3/4, d, J=2 Hz), 8.53 (1H, dd, J=2, 6 Hz)

(7) MASS (m/z): 546 (M⁺ +1); NMR (CDCl₃, δ): 1.44 (9H, s), 2.60 (3H×2/3,s), 2.82 (3H×1/3, s), 2.91-3.07 (2H, m), 3.58 (1H, dd, J=7, 16 Hz), 3.89(1H, m), 4.11-4.37 (2H, m), 4.48-4.61 (2H, m), 5.15 (1H, q, J=7 Hz),5.33 (1H, m), 6.94 (1H, m), 7.07-7.34 (16H, m)

(8) MASS (m/z): 482 (M⁺ +1); NMR (CDCl₃, δ): 0.96 (6H, m), 1.45 (9H, s),1.55-1.71 (3H, m), 2.60 (3H×2/3, s), 2.83 (3H×1/3, s), 2.98-3.03 (2H,m), 4.09 (1H×1/3, d, J=15 Hz), 4.31 (1H×1/3, d, J=15 Hz), 4.39 (1H×2/3,d, J=15 Hz), 4.56 (1H×2/3, d, J=15 Hz), 4.82 (1H, m), 5.15 (1H, m),6.82-6.96 (2H, m), 7.07-7.28 (10H, m)

(9) MASS (m/z): 547 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.85 (3H×1/3,s), 2.93 (3H×2/3, s), 3.08 (1H, m), 3.26 (1H, m), 3.56 (1H, m), 3.87(1H, m), 4.26-4.32 (2H, m), 4.46-4.67 (3H, m), 4.75 (1H, m), 5.38 (2H,m), 6.87-7.16 (4H, m), 7.24-7.53 (9H, m), 8.47 (1H, m)

(10) MASS (m/z): 500 (M+H); NMR (CDCl₃, δ): 1.41 (9H, s), 1.81-1.97 (1H,m), 1.98-2.07 (1H, m), 2.10 (3H, s), 2.46-2.55 (2H, m), 2.61 (3×2/3H,s), 2.84 (3×1/3H, s), 2.98-3.07 (2H, m), 4.09-4.43 (2×2/3H, m),4.20-4.30 (1H, m), 4.58 (2×1/3H, d, J=15 Hz), 5.12 (2H, q, J=8 Hz),6.93-7.32 (11H, m)

(11) MASS (m/z): 532 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.53(2/3×3H, z), 2.79 (1/3×3H, s), 2.85-3.04 (4H, m), 4.13 (1/3×2H, ABq,Δ=0.18, J=17 Hz), 4.22-4.38 (1H, m), 4.32 (2/3×1H, d, J=15 Hz), 4.58(2/3×1H, d, J=15 Hz), 4.90-5.18 (1H, m), 6.22 (1H, br s), 6.60-7.32(16H, m)

(12) MASS (m/z): 471 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.52(3H×1/4, s), 2.54 (3H×3/4, s), 2.68 (3H×3/4, s), 2.81 (3H×1/4, s),2.93-3.07 (2H, m), 3.41 (1H, m), 3.61 (1H, m), 4.00 (1H, m), 4.21 (1H,m), 4.41 (1H, d, J=15 Hz), 4.52 (1H, d, J=15 Hz), 5.11 (1H×3/4, m), 5.17(1H×1/4, m), 5.43 (1H, d, J=6 Hz), 7.08-7.37 (7H, m), 8.24 (1H×1/4, brs), 8.31 (1H×3/4, br s)

(13) MASS (m/z): 470 (M⁺ +1); NMR (CDCl₃, δ): 1.11 (3H×1/3, d, J=7 Hz),1.14 (3H×2/3, d, J=7 Hz), 1.46 (9H, s), 2.68 (3H×2/3, s), 2.86 (3H×1/3,s), 2.93-3.10 (2H, m), 4.03 (1H×1/3, d, J=8 Hz), 4.12 (1H×2/3, d, J=8Hz), 4.22 (1H×1/3, d, J=16 Hz), 4.25 (1H, br s), 4.41 (1H×2/3, d, J=15Hz), 4.42 (1H×1/3, d, J=16 Hz), 4.61 (1H×2/3, d, J=15 Hz), 5.15 (1H, m),5.34 (1H, m), 7.02-7.29 (12H, m)

(14) MASS: 566 (M+1); NMR (CDCl₃, δ): 1.37 (9H, s), 2.47 (3×2/3H, s),2.69 (3×1/3H, s), 2.88-3.02 (2H, m), 3.13-3.27 (2H, m), 3.09 (2×1/6H, d,J=16 Hz), 4.09 (2×1/3H, d, J=15 Hz), 4.13 (2×1/6H, d, J=16 Hz),4.40-4.52 (1H, m), 4.51 (2×1/3H, d, J=15 Hz), 4.92-5.01 (1H, m),5.02-5.13 (1H, m), 6.68 (1×1/3H, d, J=8 Hz), 6.78 (1×2/3H, d, J=8 Hz),6.81-6.90 (1H, m), 6.98-7.20 (6H, m), 7.21-7.30 (3H, m), 7.31 (1H, t,J=8 Hz), 7.40-7.48 (2H, m), 7.62 (1H, s), 7.70-7.82 (3H, m)

(15) MASS: 521 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.53 (3H, s), 2.58(3×3/4H, s), 2:72 (3×1/4H, s), 2.78-3.01 (3H, m), 3.03-3.20 (1H, m),3.95 (2×1/8H, d, J=16 Hz), 4.30 (2×1/8H, d, J=16 Hz), 4.32 (2×3/8H, d,J=15 Hz), 4.48 (2×3/8H, d, J=15 Hz), 4.32-4.50 (1H, m), 4.97-5.12 (1H,m), 5.70-5.90 (1H, m), 6.80 (1H, s), 7.02-7.40 (8H, m), 7.50 (1×4/5H,s), 7.52 (1×1/5H, s), 8.17 (1×1/5H, s), 8.27 (1×4/5H, s)

(16) MASS: 530 (M+1); NMR (CDCl₃, δ): 1.33 (9×1/2H, s), 1.37 (9×1/2H,s), 2.43-2.70 (5H, m), 2.77-3.10 (4H, m), 3.17-3.37 (1H, m), 4.29(2×1/6H, d, J=16 Hz), 4.31 (2×1/3H, d, J=15 Hz), 4.36 (2×1/6H, d, J=16Hz), 4.62 (2×1/3H, d, J=15 Hz), 4.69-4.80 (1×1/2H, m), 4.81-4.99(1×1/2H, m), 5.12-5.23 (1H, m), 6.50-6.90 (1H, m), 6.93-7.37 (15H, m)

(17) MASS: 568 (M+1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.59 (3×3/4H, s),2.83 (3×1/4H, s), 2.71-2.88 (2H, m), 3.15-3.40 (2H, m), 4.30 (2×1/6H, d,J=16 Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.43 (2×1/3H, d, J=15 Hz), 4.78(2×1/3H, d, J=15 Hz), 4.52-4.63 (1H, m), 5.03-5.20 (1H, m), 6.37-6.46(1H, m), 7.02-7.22 (7H, m), 7.51-7.80 (5H, m), 7.87 (1H, s), 8.06(1×1/4H, d, J=8 Hz), 8.10 (1×3/4H, d, J=8 Hz), 8.51 (1×3/4H, d, J=2 Hz),8.54 (1×1/4H, d, J=2 Hz), 8.70 (1H, d, J=8 Hz)

(18) MASS: 508 (M+1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.92 (3×3/4H, s),2.98 (3×1/4H, s), 3.00-3.22 (2H, m), 3.30 (1H, t, J=5 Hz), 3.52-3.64(1H, m), 3.87-4.02 (1H, m), 4.12-4.25 (1H, m), 4.68 (2×1/6H, d, J=16Hz), 4.71 (2×1/3H, d, J=15 Hz), 4.73 (2×1/6H, d, J=16 Hz), 4.98 (2×1/3H,d, J=15 Hz), 5.14-5.32 (1H, m), 5.38-5.48 (1H, m), 7.12-7.22 (6H, m),7.73-7.80 (2H, m), 7.99-8.06 (1H, m), 8.10-8.14 (1H, m), 8.78 (1×1/6H,s), 8.80 (1×5/6H, s)

(19) MASS: 569 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.73 (3×4/5H, s),2.80-3.10 (2H, m), 2.91 (3×1/5H, s), 3.12-3.40 (2H, m), 4.50-4.70 (1H,m), 4.59 (2×1/2H, d, J=15 Hz), 4.91 (2×1/2H, d, J=15 Hz), 5.03-5.28 (1H,m), 6.23-6.41 (1H, m), 7.00-7.23 (7H, m), 7.59 (1H, t, J=8 Hz),7.67-7.80 (3H, m), 7.92-8.03 (1H, m), 8.04-8.14 (1H, m), 8.48-8.52 (1H,m), 8.58 (1×1/5H, s), 8.71 (1×4/5H, s)

(20) MASS: 558 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.83 (3×4/5H, s),2.90-3.20 (5H, m), 2.98 (3×1/5H, s), 4.33-4.45 (1H, m), 4.63 (2×1/5H,s), 4.74 (2×2/5H, d, J=15 Hz), 4.83 (2×2/5H, d, J=15 Hz), 5.02-5.12(1×4/5H, m), 5.13-5.22 (1×1/5H, m), 6.81 (1H, s), 7.08-7.30 (6H, m),7.51 (1H, s), 7.73-7.80 (2H, m), 7.98-8.03 (1H, m), 8.10-8.17 (1H, m),8.72 (1×1/5H, s), 8.77 (1×4/5H, s)

(21) MASS: 534 (M+1); NMR (CDCl₃, δ): 1.48 (9H, s), 2.83 (3×3/4H, s),2.87 (3×1/4H, s), 2.95-3.12 (2H, m), 3.55-3.63 (1H, m), 3.95-4.02 (1H,m), 4.15-4.25 (1H, m), 4.42 (2×1/6H, d, J=16 Hz), 4.43 (2×1/3H, d, J=15Hz), 4.47 (2×1/6H, d, J=16 Hz), 4.70 (2×1/3H, d, J=15 Hz), 5.10-5.22(1H, m), 5.38-5.48 (1H, m), 7.08-7.32 (7H, m), 7.45 (1×1/4H, dd, J=8, 2Hz), 7.58 (1×3/4H, dd, J=8, 2 Hz), 7.81 (1H, dd, J=8, 5 Hz), 8.31-8.40(2H, m), 8.41 (1×1/4H, s), 8.50 (1×3/4H, s), 8.67-8.71 (1H, m)

(22) MASS: 595 (M+1); NMR (CDCl₃, δ): 1.44 (9H, s), 2.59 (3×4/5H, s),2.70-3.02 (2H, m), 2.68 (3×1/5H, s), 3.13-3.40 (2H, m), 4.16 (2×1/6H, d,J=16 Hz), 4.30 (2×1/6H, d, J=16 Hz), 4.37 (2×1/3H, d, J=15 Hz), 4.53(2×1/3H, d, J=15 Hz), 4.54-4.63 (1H, m), 5.01-5.13 (1H, m), 6.35-6.48(1H, m), 7.03-7.28 (7H, m), 7.37-7.47 (2H, m), 7.53-7.70 (3H, m),8.23-8.33 (1H, m), 8.47 (1H, s), 8.51 (1H, d, J=3 Hz), 8.67 (1H, d, J=8Hz), 9.18 (1H, s)

(23) MASS: 534 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.73 (3×4/5H, s),2.83 (3×1/5H, s), 2.97-3.17 (2H, m), 3.23-3.32 (1H, m), 3.58-3.66 (1H,m), 3.94-4.07 (1H, m), 4.11 (2×1/6H, d, J=16 Hz), 4.17-4.25 (1H, m),4.48 (2×1/6H, d, J=16 Hz), 4.50 (2×1/3H, d, J=15 Hz), 4.59 (2×1/3H, d,J=15 Hz), 5.10-5.22 (1H, m), 5.38-5.45 (1H, m), 7.12-7.32 (6H, m),7.38-7.48 (1H, m), 7.55 (1H, dd, J=8, 2 Hz), 7.68 (1H, dd, J=8, 2 Hz),8.27-8.32 (1H, m), 8.43 (1×1/5H, s), 8.52 (1×4/5H, s), 8.67 (1H, d, J=2Hz), 9.19 (1H, s)

(24) MASS (m/z): 737 (M⁺ +1); NMR (CDCl₃, δ): 1.42 (9H, s), 1.44 (2H,m), 1.82 (2H, m), 2.14 (3H, s), 2.66 (3H, s), 2.73 (3H, s), 2.75 (2H,m), 2.78 (3H, s), 3.12 (2H, m), 3.82 (3H, s), 4.14 (1H, d, J=16 Hz),4.41 (1H, d, J=16 Hz), 4.54 (1H, m), 4.92 (1H, m), 4.52 (1H, m), 6.55(1H, s), 7.00-7.24 (10H, m)

(25) MASS (m/z): 517 (M⁺ +1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.55(3H×3/4, s), 2.77 (3H×1/4, s), 2.97 (2H, m), 3.06 (2H, m), 4.03 (1H×1/4,d, J=16 Hz) 4.24 (1H×1/4, d, J=16 Hz), 4.32 (1H×3/4, d, J=15 Hz), 4.37(1H, m), 4.57 (1H×3/4, d, J=15 Hz), 4.92 (1H, m), 5.10 (1H, m), 6.72(1H, m), 7.10-7.39 (12H, m), 8.26 (1H×1/4, br s), 8.40 (1H×3/4, br s),8.53 (1H, m)

(26) MASS (m/z): 518 (M⁺ +1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.59(3H×3/4, s), 2.78 (3H×1/4, s), 2.92-3.03 (3H, m), 3.12 (1H, m), 3.99(1H×1/4, d, J=16 Hz), 4.27 (1H×1/4, d, J=16 Hz), 4.33 (1H×3/4, d, J=15Hz), 4.43 (1H, m), 4.61 (1H×3/4, d, J=15 Hz), 4.95 (1H, d, J=7 Hz), 5.09(1H, m), 6.90 (1H, d, J=7 Hz), 7.09-7.40 (9H, m), 8.27 (1H×1/5, br s),8.41 (1H×4/5, br s), 8.50 (2H, d, J=5 Hz), 8.53 (1H, d, J=5 Hz)

(27) MASS (m/z): 523 (M⁺ +1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.73(3H×3/4, s), 2.85 (3H×1/4, s), 2.93-3.11 (2H, m), 3.59 (1H, m), 3.98(1H, m), 4.17 (1H×1/4, d, J=15 Hz), 4.20 (1H, m), 4.47 (1H×1/4, d, J=15Hz), 4.52 (1H×3/4, d, J=15 Hz), 4.58 (1H×3/4, d, J=15 Hz), 5.14 (1H, m),5.40 (1H, m), 7.17-7.27 (7H, m), 7.61 (2H, d, J=8 Hz), 8.10 (1H, s),8.54 (1H, s)

(28) MASS (m/z): 515 (M+1)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 1.90 (1H,m), 2.03 (1H, m), 2.10 (3H, s), 2.47-2.57 (2H, m), 2.54 (3H, m), 2.60(3H×4/5, s), 2.79 (3H×1/5, s), 3.01 (2H, d, J=7.5 Hz), 4.27 (1H, m),4.36 (1H, d, J=14.5 Hz), 4.52 (1H, d, J=14.5 Hz), 5.07-5.23 (2H, m),6.90-7.01 (1H, m), 7.05-7.23 (6H, m), 7.25-7.34 (1H, m), 8.20 (1/5H, d,J=2.5 Hz), 8.31 (4/5H, d, J=2.5 Hz)

(29) MASS (m/z): 501 (M+1)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 1.91 (1H,m), 2.04 (1H, m), 2.10 (3H, s), 2.47-2.57 (2H, m), 2.63 (3H×4/5, s),2.80 (3H×1/5, s), 3.02 (2H, d, J=8.5 Hz), 4.26 (1H, m), 4.37 (1H, d,J=14.5 Hz), 4.59 (1H, d, J=14.5 Hz), 5.09-5.20 (2H, m), 6.92-7.02 (1H,m), 7.10-7.30 (6H, m), 7.39-7.45 (1H, m), 8.29 (1H×1/5, d, J=1.5 Hz),8.41 (1H×4/5, d, J=1.5 Hz), 8.53 (1H, d, J=5.5 Hz)

(30) MASS (m/z): 551 (M+1)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 1.92 (1H,m), 2.05 (1H, m), 2.09 (3H, s), 2.46-2.58 (2H, m), 2.69 (3H×4/5, s),2.88 (3H×1/5, s), 3.03 (2H, d, J=7.5 Hz), 4.21-4.35 (1H, m), 4.28(1H×1/5, d, J=14.5 Hz), 4.51 (1H×1/5, d, J=14.5 Hz), 4.56 (1H×4/5, d,J=14.5 Hz), 4.78 (1H×4/5, d, J=8.0 Hz), 5.07-5.29 (2H, m), 6.93-7.04(1H, m), 7.10-7.20 (5H, m), 7.51-7.60 (1H, m), 7.68-7.78 (1H, m), 7.80(1H, d, J=7.5 Hz), 7.93 (1H×4/5, d, J=0.75 Hz), 8.06 (1H×1/5, d, J=0.75Hz), 8.11 (1H, d, J=7.5 Hz), 8.61 (1H×1/5, d, J=1.5 Hz), 8.77 (1H×4/5,d, J=1.5 Hz)

(31) MASS (m/z): 552 (M+1)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 1.83-2.11(2H, m), 2.08 (3H, s), 2.41-2.57 (1H, m), 2.52 (1H, t, J=7.5 Hz), 2.87(3H×4/5, s), 2.96 (3H×1/5, s), 3.01-3.10 (2H, m), 4.20-4.32 (1H, m),4.61 (2H×1/5, s), 4.69 (1H×4/5, d, J=14.5 Hz), 4.93 (1H×4/5, d, J=14.5Hz), 5.08-5.29 (2H, m), 6.97 (1H, m), 7.11-7.24 (5H, m), 7.73-7.80 (2H,m), 7.97-8.04 (1H, m), 8.07-8.15 (1H, m), 8.66 (1H×1/5, s), 8.79(1H×4/5, s)

(32) MASS (m/z): 578 (M+1)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 1.86-1.97(1H, m), 2.00-2.12 (1H, m), 2.10 (3H, s), 2.52 (2H, t, J=7.5 Hz), 2.69(3H×4/5, s), 2.83 (3H×1/5, s), 3.03 (2H, d, J=7.5 Hz), 4.13 (1H×1/5, d,J=14.5 Hz), 4.39 (1H×1/5, d, J=14.5 Hz), 4.48 (1H×4/5, d, J=14.5 Hz),4.59. (1H×4/5, d, J=14.5 Hz), 5.08-5.23 (2H, m), 6.92-7.01 (1H, m),7.13-7.33 (6H, m), 7.40 (1H, dd, J=7.5, 5.5 Hz), 7.52 (1H, dd, J=8.5,1.5 Hz), 7.65 (1H×1/5, d, J=7.5 Hz), 7.69 (1H×4/5, d, J=7.5 Hz), 8.31(1H, dd, J=8.5, 1.5 Hz), 8.40 (1H×1/5, d, J=1.5 Hz), 8.52 (1H×4/5, d,J=1.5 Hz), 8.65 (1H, d, J=5.5 Hz), 9.17 (1H×1/5, d, J=1.5 Hz), 9.19(1H×4/5, d, J=1.5 Hz)

(33) MASS (m/z): 522 (M+1)⁺ ; NMR (CDCl₃, δ): 1.43 (9H, s), 2.53(3H×2/3, s), 2.80 (3H×1/3, s), 2.91-3.06 (2H, m), 3.18-3.39 (2H, m),4.00 (1H×1/3, d, J=14.5 Hz), 4.26 (1H×1/3, d, J=14.5 Hz), 4.30-4.45 (1H,br s), 4.38 (1H×2/3, d, J=14.5 Hz), 4.53 (1H×2/3, d, J=14.5 Hz), 5.00(1H, br s), 5.14 (1H, m), 6.81 (1H, dd, J=8.5, 1.5 Hz), 6.87-6.95 (2H,m), 7.07 (1H, dd, J=7.0, 1.5 Hz), 7.09-7.32 (10H, m)

(34) MASS: 500 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45 (9H, s), 2.66 (2/3×3H, s),2.78 (1/3×3H, s), 2.87-3.07 (2H, m), 3.05 (1/3×6H, s), 3.07 (2/3×6H, z),3.52-3.65 (1H, m), 3.82 (1/3×1H, d, J=17 Hz), 3.90-4.05 (1H, m),4.11-4.26 (1H, m), 4.34 (1/3×1H, d, J=17 Hz), 4.35 (2/3×2H, ABq, Δ=0.11,J=15 Hz), 5.01-5.32 (1H, m), 5.32-5.48 (1H, m), 6.47 (1H, d, J=9 Hz),7.05-7.35 (7H, m), 7.90 (1/3×1H, d, J=2 Hz), 7.98 (2/3×1H, d, J=2 Hz)

(35) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 2.68(3/4×3H, s), 2.86 (1/4×3H, s), 2.92-3.16 (2H, m), 3.53-3.66 (1H, m),3.81-4.00 (1H, m), 4.21-4.62 ((2 +1/4)H, m), 4.56 (2H, s), 4.81 (3/4×1H,d, J=15 Hz), 5.10-5.45 (2H, m), 7.03-8.16 (16H, m), 8.61 (1/4×1H, d, J=2Hz), 8.75 (3/4×1H, d, J=2 Hz)

(36) MASS (m/z): 506 (M+H)⁺ ; NMR (CDCl₃, δ): 1.43 (9H, s), 2.56(2/3×3H, s), 2.80-3.06 (4H, m), 2.82 (1/3×3H, s), 4.15 (1/3×2H, ABq,Δ=0.24, J=17 Hz), 4.20-4.39 (1H, m), 4.46 (2/3×2H, ABq, Δ=0.15, J=15Hz), 4.91 (1H, br s), 5.05-5.20 (1H, m), 6.21 (1/3×1H, s), 6.26 (2/3×1H,s), 6.70-7.40 (13H, m)

(37) MASS (m/z): 506 (M+H)⁺ ; NMR (CDCl₃, δ): 1.44 (9H, s), 2.52(2/3×3H, s), 2.78 (1/3×3H, s), 2.87-3.22 (4H, m), 4.13 (1/3×2H, ABq,Δ=0.24, J=17 Hz), 4.34-4.48 (1H, m), 4.43 (2/3×2H, ABq, Δ=0.16, J=15Hz), 5.00-5.23 (2H, m), 6.02-6.13 (1H, m), 6.27 (1H, m), 6.80-7.37 (12H,m)

(38) MASS.: 487 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.64 (3×3/4H, s),2.78 (3×1/4H, s), 2.90-3.11 (2H, m), 3.25-3.43 (1H, m), 3.52-3.63 (1H,m), 3.90 (3H, s), 3.84-4.02 (1H, m), 4.12-4.23 (1H, m), 4.23 (2×1/6H, d,J=16 Hz), 4.30 (2×1/3H, d, J=15 Hz), 4.35 (2×1/6H, d, J=16 Hz), 4.50(2×1/3H, d, J=15 Hz), 5.02-5.25 (1H, m), 5.37-5.48 (1H, m), 6.68 (1H, d,J=8 Hz), 7.07-7.40 (7H, m), 7.88 (1×1/5H, s), 7.95 (1×4/5H, s)

(39) MASS: 557 (M+1); NMR (CDCl₃, δ): 1.40 (9H, s), 2.63 (3×4/5H, s),2.84 (3×1/5H, s), 2.88-3.20 (4H, m), 4.22 (2×1/6H, d, J=16 Hz),4.33-4.50 (1H, m), 4.53 (2×1/6H, d, J=16 Hz), 4.60 (2×1/3H, d, J=15 Hz),4.68 (2×1/3H, d, J=15 Hz), 5.00-5.18 (1H, m), 5.71-5.90 (1H, m), 6.80(1H, s), 7.04-7.22 (5H, m), 7.44-7.60 (3H, m), 7.68-7.80 (2H, m), 7.90(1H, s), 8.04-8.11 (1H, m), 8.61 (1×1/5H, s), 8.71 (1×4/5H, s)

(40) MASS: 584 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.68 (3×4/5H, s),2.81 (3×1/5H, s), 2.87-3.02 (3H, m), 3.08-3.20 (1H, m), 4.11 (2×1/6H, d,J=16 Hz), 4.32-4.45 (1H, m), 4.48 (2×1/3H, d, J=15 Hz), 4.51 (2×1/3H, d,J=15 Hz), 4.58 (2×1/6H, d, J=16 Hz), 5.00-5.13 (1H, m), 6.82 (1H, s),7.08-7.16 (2H, m), 7.18-7.28 (4H, m), 7.30-7.43 (2H, m), 7.46-7.53 (2H,m), 7.62-7.70 (1H, m), 8.29 (1H, d, J=8 Hz), 8.39 (1×1/5H, s), 8.50(1×4/5H, s), 8.63 (1H, d, J=5 Hz), 9.18 (1H, s)

(41) MASS: 546 (M+1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.54 (3×2/3H, s),2.79 (3×1/3H, s), 2.90-3.03 (4H, m), 3.77 (3H, s), 4.02 (2×1/6H, d, J=16Hz), 4.23 (2×1/6H, d, J=16 Hz), 4.31 (2×1/3H, d, J=15 Hz), 4.58 (2×1/3H,d, J=15 Hz), 4.25-4.40 (1H, m), 4.87-4.98 (1H, m), 5.03-5.18 (1H, m),6.63-6.93 (4H, m), 7.01-7.17 (5H, m), 7.17-7.21 (2H, m), 7.22-7.32 (4H,m)

(42) MASS: 569 (M+1); NMR (CDCl₃, δ): 1.48 (9H, s), 2.60 (3×2/3H, s),2.82 (3×1/3H, s), 2.73-2.90 (2H, m), 3.17-3.42 (2H, m), 4.40 (2×1/6H, d,J=16 Hz), 4.55 (2×1/6H, d, J=16 Hz), 4.56 (2×1/3H, d, J=15 Hz),4.56-4.67 (1H, m), 4.75 (2×1/3H, d, J=15 Hz), 5.08-5.19 (1H, m),6.30-6.50 (1H, m), 7.07-7.23 (7H, m), 7.38 (1H, d, J=8 Hz), 7.60 (1H, t,J=8 Hz), 7.62-7.75 (1H, m), 7.81 (1×2/3H, s), 8.01 (1×1/3H, s), 7.99(1H, d, J=8 Hz), 8.51 (1H, d, J=3 Hz), 8.82 (2H, s)

(43) MASS: 566 (M+1); NMR (CDCl₃, δ): 1.38 (9H, s), 2.43 (3×3/4H, s),2.71 (3×1/4H, s), 2.80-2.98 (2H, m), 3.35-3.67 (2H, m), 4.03 (2×1/8H, d,J=16 Hz), 4.16 (2×1/8H, d, J=16 Hz), 4.18 (2×3/8H, d, J=15 Hz), 4.54(2×3/8H, d, J=15 Hz), 4.42-4.53 (1H, m), 4.90-5.18 (2H, m), 6.50-6.65(1H, m), 6.83-7.40 (12H, m), 7.42-7.60 (2H, m), 7.74 (1H, d, J=8 Hz),7.83 (1H, t, J=8 Hz), 8.12 (1H, d, J=8 Hz)

(44) MASS: 507 (M+1); NMR (CDCl₃, δ): 1.44 (9H, s), 2.60 (3×3/4H, s),2.71 (3×1/4H, s), 2.74-3.03 (3H, m), 3.04-3.19 (1H, m), 4.32-4.40 (1H,m), 4.41 (2×3/8H, d, J=15 Hz), 4.47 (2×3/8H, d, J=15 Hz), 4.50 (2×1/8H,d, J=16 Hz), 4.63 (2×1/8H, d, J=16 Hz), 4.99-5.12 (1H, m), 5.72-5.90(1H, m), 6.81 (1H, s), 7.08-7.32 (7H, m), 7.32-7.43 (1H, m), 7.47-7.53(1H, m), 8.27 (1×1/4H, s), 8.38 (1×3/4H, s), 8.49-8.53 (1H, m)

(45) MASS: 532 (M+1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.49 (3H, s), 2.52(3×3/4H, s), 2.71 (3×1/4H, s), 2.87-3.00 (2H, m), 3.14-3.41 (2H, m),3.98 (2×1/8H, d, J=16 Hz), 4.20 (2×1/8H, d, J=16 Hz), 4.23 (2×3/8H, d,J=15 Hz), 4.50 (2×3/8H, d, J=15 Hz), 4.52-4.63 (1H, m), 5.00-5.17 (1H,m), 6.30-6.47 (1H, m), 6.92-7.30 (9H, m), 7.53-7.68 (2H, m), 8.12(1×1/4H, s), 8.25 (1×3/4H, s), 8.48-8.52 (1H, m)

(46) MASS: 517 (M+1); NMR (CDCl₃, δ): 1.40 (9H, s), 2.58 (3×2/3H, s),2.82 (3×1/3H, s), 2.83-3.19 (4H, m), 4.09 (2×1/6H, d, J=15 Hz), 4.30(2×1/6H, d, J=15 Hz), 4.33 (2×1/3H, d, J=16 Hz), 4.33-4.50 (1H, m), 4.60(2×1/3H, d, J=16 Hz), 5.00-5.20 (2H, m), 6.90-7.40 (12H, m), 7.50 (1H,t, J=8 Hz), 8.40 (1H, s), 8.48 (1H, s)

(47) MASS: 550 (M+1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.57 (3×2/3H, s),2.81 (3×1/3H, s), 2.87-3.10 (4H, m), 3.99 (2×1/6H, d, J=16 Hz), 4.27(2×1/6H, d, J=16 Hz), 4.32 (2×1/3H, d, J=15 Hz), 4.60 (2×1/3H, d, J=15Hz), 4.28-4.43 (1H, m), 4.85-5.00 (1H, m), 5.02-5.18 (1H, m), 6.69-6.99(2H, m), 7.02-7.15 (5H, m), 7.16-7.40 (8H, m)

(48) MASS: 528 (M+1); NMR (CDCl₃, δ): 1.46 (9×2/3H, s), 1.50 (9×1/3H,s), 2.48-2.73 (2H, m), 2.51 (3×2/3H, s), 2.78 (3×1/3H, s), 2.90-3.37(2H, m), 4.26-4.70 (4H, m), 4.82-5.10 (2H, m), 6.52-6.73 (1H, m),6.83-7.08 (5H, m), 7.09-7.40 (9H, m)

Preparation 61

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8, 41 or 54.

(1) NMR (CDCl₃, δ): 1.99 (3×1/3H, s), 2.03 (3×2/3H, s), 2.38-2.58 (1H,m), 2.72 (3×2/3H, s), 2.82-3.12 (3H, m), 2.90 (3×1/3H, s), 3.38 (1×1/3H,dd, J=12, 4 Hz), 3.49 (1×2/3H, dd, J=12, 4 Hz), 4.35 (2×2/3H, d, J=15Hz), 4.36 (2×1/6H, d, J=16 Hz), 4.43 (2×1/6H, d, J=16 Hz), 4.68 (2×1/3H,d, J=15 Hz), 5.19 (1H, q, J=12 Hz), 7.00-7.32 (10H, m), 8.04 (1×1/3H, d,J=8 Hz), 8.13 (1×2/3H, d, J=8 Hz)

(2) MASS: 391 (M+1); NMR (CDCl₃, δ): 2.71 (3×3/4H, s), 2.79 (3×1/4H, s),2.93-3.17 (2H, m), 3.35-3.49 (1H, m), 3.58-3.68 (1H, m), 3.70-3.81 (1H,m), 4.20 (2×1/8H, d, J=16 Hz), 4.39 (2×1/8H, d, J=16 Hz), 4.35 (2×3/8H,d, J=15 Hz), 4.58 (2×3/8H, d, J=15 Hz), 5.12 (1H, q, J=8 Hz), 7.10-7.18(2H, m), 7.20-7.30 (4H, m), 7.38 (1H, d, J=8 Hz), 7.97 (1H, d, J=8 Hz),8.09 (1×1/4H, s), 8.19 (1×3/4H, s)

(3) MASS: 614 (M+1); NMR (CDCl₃, δ): 2.31-2.50 (1H, m), 2.57-2.68 (1H,m), 2.63 (3×2/3H, s), 2.81 (3×1/3H, s), 2.88-3.04 (3H, m), 4.28 (2×2/3H,d, J=15 Hz), 4.63 (2×1/3H, d, J=15 Hz), 5.09 (1H, q, J=8 Hz), 6.93-7.31(19H, m), 7.40-7.45 (6H, m), 7.70 (1×1/3H, d, J=8 Hz), 7.80 (1×2/3H, d,J=8 Hz)

(4) MASS: 407 (M+1); NMR (CDCl₃, δ): 2.73 (3×3/4H, s), 2.89 (3×1/4H, s),2.94-3.18 (2H, m), 3.38-3.86 (3H, m), 4.39 (2×1/6H, d, J=16 Hz), 4.59(2×1/6H, d, J=16 Hz), 4.60 (2×1/3H, d, J=15 Hz), 4.73 (2×1/3H, d, J=15Hz), 5.11-5.31 (1H, m), 7.08-7.28 (5H, m), 7.56 (1H, t, J=8 Hz), 7.69(1H, t, J=8 Hz), 7.77 (1H, d, J=8 Hz), 7.90 (1H, s), 8.00-8.12 (2H, m),8.68 (1×1/4H, d, J=2 Hz), 8.74 (1×3/4H, d, J=2 Hz)

(5) NMR (CDCl₃, δ): 2.55 (3H×2/3, s), 2.73 (3H×1/3, s), 3.00 (2H, t, J=7Hz), 3.88 (2H, m), 4.06-4.61 (5H, m), 5.12 (1H, d, J=7 Hz), 6.84-7.25(15H, m), 8.14 (1H, d, J=7 Hz)

(6) NMR (CDCl₃, δ): 0.88 (6H, m), 1.57-1.85 (3H, m), 2.62 (3H×2/3, s),2.80 (3H×1/3, s), 2.95-3.14 (2H, m), 4.15 (1H, m), 4.18 (1H×1/3, d, J=15Hz), 4.27 (1H×2/3, d, J=15 Hz), 4.32 (1H×1/3, d, J=15 Hz), 4.58 (1H×2/3,d, J=15 Hz), 5.18 (1H, t, J=7 Hz), 6.90-6.99 (3H, m), 7.11-7.23 (7H, m),8.14 (1H×2/3, d, J=8 Hz), 8.22 (1H×1/3, d, J=8 Hz)

(7) NMR (CD₃ OD, δ): 2.90 (3H×2/3, s), 3.04 (3H×1/3, s), 3.41 (1H, m),3.56 (1H, m), 3.65-3.73 (2H, m), 3.80 (1H, m), 4.13 (1H, m), 4.37-4.67(4H, m), 5.47 (1H, m), 7.18-7.37 (8H, m), 7.76 (1H, m), 7.89-8.02 (2H,m), 8.26 (1H, m), 8.48 (1H, m), 8.73 (1H, m)

(8) NMR (CDCl₃, δ): 2.81 (3H×3/4, s), 2.89 (3H×1/4, s), 2.92-3.14 (2H,m), 3.29 (1H×1/4, t, J=5 Hz), 3.44 (1H×3/4, t, J=5 Hz), 3.52-3.64 (1H,m), 3.72-3.83 (1H, m), 4.37 (1H×1/4, d, J=15 Hz), 4.41 (1H×3/4, d, J=15Hz), 4.47 (1H×1/4, d, J=15 Hz), 4.62 (1H×3/4, d, J=15 Hz), 5.04 (1H×1/4,q, J=5 Hz), 5.21 (1H×3/4, q, J=5 Hz), 6.88 (2H×1/4, d, J=7 Hz), 6.94(2H×3/4, d, J=7 Hz), 7.11-7.28 (5H, m), 7.92 (1H, d, J=5 Hz), 8.51 (2H,d, J=7 Hz)

(9) NMR (CDCl₃, δ): 2.45 (1H×1/3, dd, J=8, 15 Hz), 2.60 (1H×2/3, dd,J=8, 15 Hz), 2.70 (3H×2/3, s), 2.85 (3H×1/3, s), 2.91-3.22 (3H, m), 3.50(1H×1/3, dd, J=4, 8 Hz), 3.59 (1H×2/3, dd, J=4, 8 Hz), 4.32 (1H×2/3, d,J=15 Hz), 4.33 (1H×1/3, d, J=15 Hz), 4.42 (1H×1/3, d, J=15 Hz), 4.67(1H×2/3, d, J=15 Hz), 5.22 (1H, m), 6.97-7.34 (15H, m), 7.92 (1H×1/3, d,J=8 Hz), 8.00 (1H×2/3, d, J=8 Hz)

(10) NMR (CD₃ OD, δ): 2.93 (3H×3/4, s), 3.07 (2H, d, J=7 Hz), 3.34(3H×1/4, s), 3.85 (1H, dd, J=7, 12 Hz), 3.93-4.01 (2H, m), 4.41 (1H×1/4,d, J=15 Hz), 4.53 (1H×3/4, d, J=15 Hz), 4.75 (1H×1/4, d, J=15 Hz), 4.81(1H×3/4, d, J=15 Hz), 5.11 (1H, t, J=7 Hz), 7.24-7.31 (5H, m), 8.02 (1H,dd, J=6, 8 Hz), 8.30 (1H, d, J=8 Hz), 8.67 (1H, d, J=2 Hz), 8.77 (1H, d,J=6 Hz)

(11) MASS (m/z): 400 (M+H); NMR (CDCl₃, δ): 1.62-1.78 (1H, m), 1.90-2.02(1H, m), 2.05 (3×1/3H, s), 2.09 (3×2/3H, s), 2.42 (1H, t, J=8 Hz), 2.51(1H, t, J=8 Hz), 2.70 (3×2/3H, s), 2.90 (3×1/3H, s), 2.97-3.11 (2H, m),3.38-3.41 (1×1/3H, m), 3.47-3.51 (1×2/3H, m), 4.31-4.39 (2×2/3H, m),4.69 (2×1/3H, d, J=15 Hz), 5.19 (1H, q, J=8 Hz), 7.01-7.32 (10H, m),7.83 (1×1/3H, d, J=8 Hz), 7.91 (1×2/3H, d, J=8 Hz)

(12) MASS (m/z): 356 (M+1); NMR (CDCl₃, δ): 2.73 (3×2/3H, s), 2.89(3×1/3H, s), 2.92-3.12 (2H, m), 3.30 (1×1/3H, t, J=8 Hz), 3.42 (1H×2/3H,t, J=8 Hz), 3.48-3.62 (1H, m), 3.67-3.81 (1H, m), 4.31-4.51 (2×2/3H, m),4.69 (2×1/3H, d, J=15 Hz), 5.19 (1H, q, J=8 Hz), 7.06 (2×1/3H, d, J=8Hz), 7.11 (2×2/3H, d, J=8 Hz), 7.13-7.33 (8H, m), 7.82-7.93 (1H, m)

(13) NMR (CDCl₃, δ): 2.52 (3H×1/4, s), 2,54 (3H×3/4, s), 2.72 (3H×3/4,s), 2.82 (3H×1/4, s), 2.93-3.09 (2H, m), 3.36 (1H×1/4, t, J=6 Hz), 3.42(1H×3/4, t, J=6 Hz), 3.61 (1H, m), 3.77 (1H, m), 4.15 (1H×1/4, d, J=16Hz), 4.37 (1H×3/4, d, J=15 Hz), 4.42 (1H×1/4, d, J=16 Hz), 4.56 (1H×3/4,d, J=15 Hz), 5.15 (1H×3/4, q, J=7 Hz), 5.20 (1H×1/4, q, J=7 Hz),7.05-7.35 (7H, m), 7.93 (1H, d, J=7 Hz), 8.23 (1H×1/4, d, J=2 Hz), 8.31(1H×3/4, d, J=2 Hz)

(14) NMR (CDCl₃, δ): 1.05 (3H×1/3, d, J=7 Hz), 1.12 (3H×2/3, d, J=7 Hz),2.77 (3H×2/3, s), 2.92 (3H×1/3, s), 2.94-3.12 (2H, m), 4.12 (1H, m),4.37 (1H×1/3, d, J=16 Hz), 4.39 (1H×2/3, d, J=15 Hz), 4.45 (1H, m), 4.60(1H×1/3, d, J=16 Hz), 4.67 (1H×2/3, d, J=15 Hz), 5.13 (1H×1/3, q, J=7Hz), 5.22 (1H×2/3, q, J=7 Hz), 7.05-7.31 (10H, m), 7.97 (1H, m)

(15) MASS: 466 (M+1); NMR (CDCl₃, δ): 2.58-2.83 (1H, m), 2.68 (3×2/3H,s), 2.81 (3×1/3H, s), 2.90-3.10 (2H, m), 3.28 (1×1/3H, dd, J=15, 5 Hz),3.33 (1×2/3H, dd, J=15, 5 Hz), 3.60 (1×1/3H, dd, J=12, 5 Hz), 3.70(1×2/3H, dd, J=12, 5 Hz), 4.28 (2×1/3H, d, J=15 Hz), 4.32 (2×1/6H, d,J=16 Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.68 (2×1/3H, d, J=15 Hz),5.18-5.28 (1H, m), 7.00 (2×1/3H, d, J=7 Hz), 7.07 (2×2/3H, d, J=7 Hz),7.10-7.39 (9H, m), 7.41-7.51 (2H, m), 7.61 (1×1/3H, s), 7.64 (1×2/3H,s), 7.73-7.85 (3H, m), 7.92 (1×1/3H, d, J=8 Hz), 8.01 (1×2/3H, d, J=8Hz)

(16) MASS: 421 (M+1); NMR (CDCl₃, δ): 2.50 (3H, s), 2.63 (3×3/4H, s),2.80 (3×1/4H, s), 2.82-3.10 (4H, m), 3.50-3.62 (1H, m), 4.11 (2×1/8H, d,J=16 Hz), 4.39 (2×1/8H, d, J=16 Hz), 4.41 (2×3/8H, d, J=15 Hz), 4.49(2×3/8H, d, J=15 Hz), 5.07-5.23 (1H, m), 6.81 (1H, s), 7.03-7.37 (7H,m), 7.53 (1H, s), 7.95-8.08 (1H, m), 8.22 (1×1/4H, s), 8.30 (1×3/4H, s)

(17) MASS: 430 (M+1); NMR (CDCl₃, δ): 2.26 (3H, s), 2.43-2.61 (1H, m),2.71 (3×2/3H, s), 2.86 (3×1/3H, s), 2.90-3.21 (4H, m), 4.37 (2×1/6H, d,J=16 Hz), 4.40 (2×1/3H, d, J=15 Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.61(2×1/3H, d, J=15 Hz), 5.18-5.28 (1H, m), 7.00-7.38 (15H, m), 7.80(1×1/3H, d, J=8 Hz), 7.88 (1×2/3H, d, J=8 Hz)

(18) MASS: 468 (M+1); NMR (CDCl₃, δ): 2.72 (3×2/3H, s), 2.82-3.12 (3H,m), 2.88 (3×1/3H, s), 3.19-3.32 (1H, m), 3.69 (1×1/4H, dd, J=8, 2 Hz),3.80 (1×3/4H, dd, J=8, 2 Hz), 4.51 (2×1/3H, d, J=15 Hz), 4.52 (2×1/6H,d, J=16 Hz), 4.59 (2×1/6H, d, J=16 Hz), 4.81 (2×1/3H, d, J=15 Hz),5.12-5.30 (1H, m), 7.10-7.23 (7H, m), 7.51-7.80 (4H, m), 7.92 (1H, s),8.09 (1×1/4H, d, J=8 Hz), 8.11 (1×3/4H, d, J=8 Hz), 8.22 (1×1/4H, d, J=8Hz), 8.24 (1×3/4H, d, J=8 Hz), 8.49-8.56 (1H, m), 8.63 (1×1/4H, d, J=2Hz), 8.74 (1×3/4H, d, J=2 Hz)

(19) mp: 165-167° C. MASS: 408 (M+1); NMR (CDCl₃, δ): 2.96 (3H, s),2.98-3.35 (2H, m), 3.42-3.82 (3H, m), 4.72 (2×1/6H, d, J=16 Hz), 4.73(2×1/3H, d, J=15 Hz), 4.82 (2×1/6H, d, J=16 Hz), 4.93 (2×1/3H, d, J=15Hz), 5.15-5.32 (1H, m), 7.10-7.23 (5H, m), 7.72-7.80 (2H, m), 7.90-8.03(2H, m), 8.06-8.13 (1H, m), 8.73 (1×1/5H, s), 8.80 (1×4/5H, s)

(20) MASS: 469 (M+1); NMR (CDCl₃, δ): 2.73-3.09 (2H, m), 2.91 (3×4/5H,s), 2.97 (3×1/5H, s), 3.11-3.30 (2H, m), 3.67 (1×1/5H, dd, J=8, 4 Hz),3.79 (1×4/5H, dd, J=8, 4 Hz), 4.67 (2×1/3H, d, J=15 Hz), 4.68 (2×1/6H,d, J=16 Hz), 4.89 (2×1/6H, d, J=16 Hz), 4.93 (2×1/3H, d, J=15 Hz),5.16-5.31 (1H, m), 7.08-7.22 (7H, m), 7.52-7.63 (1H, m), 7.72-7.80 (2H,m), 7.97-8.03 (1H, m), 8.08-8.14 (1H, m), 8.17-8.26 (1H, m), 8.48-8.53(1H, m), 8.68 (1×1/5H, s), 8.76 (1×4/5H, s)

(21) MASS: 458 (M+1); NMR (CDCl₃, δ): 2.70-3.20 (3H, m), 2.91 (3×3/4H,s), 2.98 (3×1/4H, s), 3.45-3.65 (2H, m), 4.70 (2×1/6H, d, J=16 Hz), 4.73(2×1/3H, d, J=15 Hz), 4.83 (2×1/6H, d, J=16 Hz), 4.89 (2×1/3H, d, J=15Hz), 5.12-5.32 (1H, m), 4.72 (1×1/4H, s), 4.89 (1×3/4H, s), 6.72(1×1/4H, s), 6.80 (1×3/4H, s), 7.05-7.23 (5H, m), 7.49 (1×1/4H, s), 7.52(1×3/4H, s), 7.71-7.80 (2H, m), 7.96-8.07 (1H, m), 8.08-8.13 (1H, m),8.72 (1×1/4H, s), 8.78 (1×3/4H, s)

(22) MASS: 434 (M+1); NMR (CDCl₃, δ): 2.78 (3×2/3H, s), 2.89 (3×1/3H,s), 2.96-3.18 (2H, m), 3.33 (1×1/3H, t, J=8 Hz), 3.42 (1×2/3H, t, J=8Hz), 3.52-3.67 (1H, m), 3.71-3.81 (1H, m), 4.35 (2×1/6H, d, J=16 Hz),4.42 (2×1/3H, d, J=15 Hz), 4.51 (2×1/6H, d, J=16 Hz), 4.71 (2×1/3H, d,J=15 Hz), 5.11-5.19 (1H, m), 7.11-7.33 (6H, m), 7.56 (1H, dd, J=8, 2Hz), 7.81 (1H, t, J=8 Hz), 7.94 (1H, d, J=8 Hz), 8.29-8.42 (2H, m), 8.49(1H, s), 8.63-8.70 (1H, m)

(23) MASS: 495 (M+1); NMR (CDCl₃, δ): 2.77 (3×4/5H, s), 2.81 (3×1/5H,s), 2.86-3.14 (3H, m), 3.20-3.32 (1H, m ), 3.70-3.82 (1H, m), 4.35(2×1/6H, d, J=16 Hz), 4.40 (2×1/3H, d, J=15 Hz), 4.43 (2×1/6H, d, J=16Hz), 4.63 (2×1/3H, d, J=15 Hz), 5.11-5.23 (1H, m), 7.10-7.32 (7H, m),7.40 (1H, dd, J=8, 4 Hz), 7.48 (1H, dd, J=8, 2 Hz), 7.56-7.70 (2H, m),8.18-8.32 (2H, m), 8.40 (1×1/5H, s), 8.49 (1×4/5H, s), 8.51 (1H, d, J=2Hz), 8.63 (1H, d, J=8 Hz), 8.19 (1H, s)

(24) MASS: 434 (M+1); NMR (CDCl₃, δ): 2.79 (3×3/4H, s), 2.88 (3×1/4H,s), 2.96-3.18 (2H, m), 3.33-3.45 (1H, m), 3.52-3.67 (1H, m), 3.74-3.83(1H, m), 4.30 (2×1/6H, d, J=16 Hz), 4.48 (2×1/3H, d, J=15 Hz), 4.49(2×1/6H, d, J=16 Hz), 4.66 (2×1/3H, d, J=15 Hz), 5.12-5.25 (1H, m),7.12-7.30 (4H, m), 7.38-7.43 (2H, m), 7.55 (1H, dd, J=8, 2 Hz), 7.68(1H, t, J=8 Hz), 7.92 (1H, d, J=8 Hz), 8.29-8.33 (1H, m), 8.44 (1×1/4H,s), 8.53 (1×3/4H, s), 8.67 (1H, d, J=5 Hz), 9.16-9.20 (1H, m)

(25) MASS (m/z): 637 (M⁺ +1);

(26) NMR (CDCl₃, δ): 2.52 (1H×1/4, dd, J=8, 14 Hz), 2.65 (1H×3/4, dd,J=8, 14 Hz), 2.70 (3H×3/4, s), 2.82 (3H×1/4, s), 3.01 (2H, m), 3.15(1H×1/4, dd, J=4, 14 Hz), 3.21 (1H×3/4, dd, J=4, 14 Hz), 3.53 (1H×1/4,dd, J=4, 8 Hz), 3.60 (1H×3/4, dd, J=4, 8 Hz), 4.29 (1H×1/4, d, J=16 Hz),4.32 (1H×3/4, d, J=15 Hz), 4.40 (1H×1/4, d, J=16 Hz), 4.66 (1H×3/4, d,J=15 Hz), 5.17 (1H, q, J=7 Hz), 7.13-7.40 (12H, m), 7.98 (1H, m), 8.30(1H×1/4, d, J=2 Hz), 8.41 (1H×3/4, d, J=2 Hz), 8.52 (1H, m)

(27) NMR (CDCl₃, δ): 2.53-2.67 (1H, m), 2.71 (3H×3/4, s), 2.83 (3H×1/4,s), 2.94-3.21 (3H, m), 3.56 (1H×1/3, dd, J=4, 9 Hz), 3.64 (1H×2/3, dd,J=4, 12 Hz), 4.25 (1H×1/4, d, J=16 Hz), 4.34 (1H×3/4, d, J=15 Hz), 4.42(1H×1/4, d, J=16 Hz), 4.64 (1H×3/4, d, J=15 Hz), 5.17 (1H, m), 7.08-7.42(9H, m), 7.97 (1H, d, J=8 Hz), 8.31 (1H×1/4, br s), 8.43 (1H×3/4, br s),8.53 (2H, d, J=5 Hz)

(28) NMR (CDCl₃, δ): 2.78 (3H×3/4, s), 2.88 (3H×1/4, s), 2.99 (1H, m),3.11 (1H, m), 3.36 (1H×1/4, t, J=5 Hz), 3.43 (1H×3/4, t, J=5 Hz), 3.58(1H, m), 3.78 (1H, m), 4.35 (1H×1/4, d, J=15 Hz), 4.47 (1H×3/4, d, J=15Hz), 4.48 (1H×1/4, d, J=15 Hz), 4.66 (1H×3/4, d, J=15 Hz), 7.13-7.28(7H, m), 7.60 (2H, d, J=8 Hz), 7.93 (1H, d, J=8 Hz), 8.11 (1H, s), 8.53(1H, s)

(29) mp: 96-99° C.; MASS (m/z): 415 (M+1)⁺ ; NMR (CDCl₃, δ): 1.70 (1H,m), 2.05 (1H, m), 2.07 (3H×1/4, s), 2.09 (3H×3/4, s), 2.43-2.58 (2H, m),2.52 (3H×1/4, s), 2.55 (3H×3/4, s), 2.70 (3H×3/4, s), 2.81 (3H×1/4, s),2.92-3.15 (2H, m), 3.38-3.52 (1H, m), 4.21 (1H×1/4, d, J=14.5 Hz), 4.32(1H×3/4, d, J=14.5 Hz), 4.39 (1H×1/4, d, J=14.5 Hz), 4.60 (1H×3/4, d,J=14.5 Hz), 5.10-5.27 (1H, m), 7.01-7.10 (1H, m), 7.11-7.34 (6H, m),7.90 (1H, d, J=9.0 Hz), 8.21 (1H×1/4, d, J=1.5 Hz), 8.30 (1H×3/4, d,J=1.5 Hz)

(30) MASS (m/z): 401 (M+1)⁺ ; NMR (CDCl₃, δ): 1.73 (1H, m), 2.07(3H×1/4, s), 2.10 (3H×3/4, s), 1.99-2.16 (1H, m), 2.48 (2H×1/4, t, J=7.5Hz), 2.53 (2H×3/4, t, J=7.5 Hz), 2.72 (3H×3/4, s), 2.84 (3H×1/4, s),2.94-3.12 (2H, m), 3.38-3.44 (1H×1/4, m), 3.46-3.52 (1H×3/4, m), 4.31(1H×1/4, d, J=14.5 Hz), 4.35 (1H×3/4, d, J=14.5 Hz), 4.41 (1H×1/4, d,J=14.5 Hz), 4.65 (1H×3/4, d, J=14.5 Hz), 5.12-5.23 (1H, m), 7.12-7.30(8H, m), 7.38-7.44 (1H, m), 7.93 (1H, d, J=8.5 Hz), 8.31 (1H×1/4, d,J=1.5 Hz), 8.43 (1H×3/4, d, J=1.5 Hz), 8.49-8.56 (1H, m)

(31) MASS (m/z): 451 (M+1)⁺ ; NMR (CDCl₃, δ): 1.65-1.79 (1H, m),1.98-2.14 (1H, m), 2.05 (3H×1/4, s), 2.10 (3H×3/4, s), 2.47 (2H×1/4, t,J=7.5 Hz), 2.53 (2H×3/4, t, J=7.5 Hz), 2.78 (3H×3/4, s), 2.92 (3H×1/4,s), 2.96-3.17 (2H, m), 3.39 (1H×1/4, dd, J=7.5, 4.5 Hz), 3.50 (1H×3/4,dd, J=7.5, 4.5 Hz), 4.52 (1H×1/4, d, J=14.5 Hz), 4.53 (1H×3/4, d, J=14.5Hz), 4.62 (1H×1/4, d, J=14.5 Hz), 4.82 (1H×3/4, d, J=14.5 Hz), 5.13-5.32(1H, m), 7.11-7.25 (5H, m), 7.51-7.60 (1H, m), 7.67-7.98 (4H, m), 8.09(1H×1/4, d, J=7.5 Hz), 8.11 (1H×3/4, d, J=7.5 Hz), 8.66 (1H×1/4, d,J=1.5 Hz), 8.78 (1H×3/4, d, J=1.5 Hz)

(32) mp: 110-111° C.; MASS (m/z): 452 (M+1)⁺ ; NMR (CDCl₃, δ): 1.63-1.78(1H, m), 1.99-2.12 (1H, m), 2.02 (3H×1/5, s), 2.08 (3H×4/5, s), 2.39(2H×1/5, t, J=7.5 Hz), 2.52 (2H×4/5, t, J=7.5 Hz), 2.94 (3H×4/5, s),2.97-3.28 (2H, m), 3.01 (3H×1/5, s), 3.38 (1H×1/5, dd, J=7.5, 5.5 Hz),3.50 (1H×4/5, dd, J=7.5, 5.5 Hz), 4.69 (1H, d, J=14.5 Hz), 4.95 (1H×1/5,d, J=14.5 Hz), 4.98 (1H×4/5, d, J=14.5 Hz), 5.17-5.33 (1H, m), 7.11-7.23(5H, m ), 7.74-7.81 (2H, m), 7.87-7.96 (1H, m), 7.99-8.04 (1H, m),8.08-8.15 (1H, m), 8.70 (1H×1/5, s), 8.80 (1H×4/5, s)

(33) MASS (m/z): 478 (M+1)⁺ ; NMR (CDCl₃, δ): 1.63-1.80 (1H, m),1.99-2.14 (1H, m), 2.08 (3H×1/4, s), 2.10 (3H×3/4, s), 2.49 (2H×1/4, t,J=7.5 Hz), 2.53 (2H×3/4, t, J=7.5 Hz), 2.78 (3H×3/4, s), 2.88 (3H×1/4,s), 2.93-3.20 (2H, m), 3.44 (1H×1/4, dd, J=7.5, 4.5 Hz), 3.51 (1H×3/4,dd, J=7.5, 4.5 Hz), 4.37 (1H×1/4, d, J=14.5 Hz), 4.43 (1H×1/4, d, J=14.5Hz), 4.47 (1H×3/4, d, J=14.5 Hz), 4.67 (1H×3/4, d, J=14.5 Hz), 5.13-5.27(1H, m), 7.14-7.38 (21/4H, m), 7.41 (1H, dd, J=8.5, 5.5 Hz), 7.51(1H×3/4, dd, J=8.5, 1.5 Hz), 7.65 (1H×1/4, d, J=7.5 Hz), 7.68 (1H×3/4,d, J=7.5 Hz), 7.88-8.01 (1H, m), 8.31 (1H, dd, J=8.5, 1.5 Hz), 8.42(1H×1/4, d, J=1.5 Hz), 8.53 (1H×3/4, d, J=1.5 Hz), 8.67 (1H, d, J=5.5Hz), 9.17 (1H×1/4, d, J=1.5 Hz), 9.20 (1H×3/4, d, J=1.5 Hz)

(34) MASS (m/z): 422 (M+1)⁺ ; NMR (CDCl₃, δ): 2.69 (3H×2/3, s), 2.87(3H×1/3, s), 2.93-3.09 (3H, m), 3.26 (1H×1/3, dd, J=14.5, 4.5 Hz), 3.31(1H×2/3, dd, J=14.5, 4.5 Hz), 3.49 (1H×1/3, dd, J=8.5, 4.5 Hz), 3.59(1H×2/3, dd, J=8.5, 4.5 Hz), 4.29 (1H×1/3, d, J=14.5 Hz), 4.33 (1H×2/3,d, J=14.5 Hz), 4.40 (1H×1/3, d, J=14.5 Hz), 4.67 (1H×2/3, d, J=14.5 Hz),5.20 (1H, q, J=7.5 Hz), 6.78-7.02 (3H, m), 7.05-7.33 (10H, m), 7.94(1H×1/3, br d, J=8.5 Hz), 8.02 (1H×2/3, br d, J=8.5 Hz)

(35) MASS (m/z): 400 (M+H)⁺ ; NMR (CDCl₃, δ): 2.69 (2/3×3H, s), 2.81(1/3×3H, s), 2.86-3.10 (2H, m), 3.06 (1/3×6H, s), 3.08 (2/3×6H, s),3.34-3.82 (3H, m), 3.92 (1/3×1H, d, J=17 Hz), 4.35 (2/3×2H, ABq, Δ=0.15,J=15 Hz), 4.36 (1/3×1H, d, J=17 Hz), 5.02-5.35 (1H, m), 6.44 (1/3×1H, d,J=9 Hz), 6.47 (2/3×1H, d, J=9 Hz), 7.06-7.36 (6H, m), 7.80-8.04 (2H, m)

(36) MASS (m/z): 497 (M+H)⁺ ; NMR (CDCl₃, δ): 2.74 (3/4×3H, s), 2.90(1/4×3H, s), 2.92-3.20 (2H, m), 3.44-3.75 (3H, m), 4.42-4.88 (4H, m),5.10-5.30 (1H, m), 7.03-8.23 (16H, m), 8.62 (1/4×1H, d, J=2 Hz), 8.77(3/4×1H, d, J=2 Hz)

(37) MASS (m/z): 406 (M+H)⁺ ; NMR (CDCl₃, δ): 2.46-2.69 (1H, m), 2.68(2/3×3H, s), 2.77-3.10 (3H, m), 2.87 (1/3×3H, s), 3.38-3.58 (1H, m),4.33 (2/3×1H, d, J=15 Hz), 4.36 (1/3×2H, ABq, Δ=0.10, J=17 Hz), 4.67(2/3×1H, d, J=15 Hz), 5.12-5.26 (1H, m), 6.21 (1/3×1H, s), 6.27 (2/3×1H,s), 6.95-7.40 (12H, m), 7.86-8.05 (1H, m)

(38) MASS (m/z): 406 (M+H)⁺ ; NMR (CDCl₃, δ): 2.61-2.84 (1H, m), 2.66(2/3×3H, s), 2.86 (1/3×3H, s), 2.89-3.20 (3H, m), 3.50-3.68 (1H, m),4.32 (2/3×1H, d, J=15 Hz), 4.34 (1/3×2H, ABq, Δ=0.22, J=17 Hz), 4.67(2/3×1H, d, J=15 Hz), 5.12-5.26 (1H, m), 6.04 (1/3×1H, d, J=2 Hz), 6.10(2/3×1H, d, J=2 Hz), 6.24-6.32 (1H, m), 6.93-7.38 (11H, m), 7.98(1/3×1H, d, J=8 Hz), 8.05 (2/3×1H, d, J=8 Hz)

(39) MASS: 387 (M+1); NMR (CDCl₃, δ): 2.71 (3×3/4H, s), 2.81 (3×1/4H,s), 2.90-3.13 (2H, m), 3.33-3.43 (1H, m), 3.51-3.61 (1H, m), 3.70-3.81(1H, m), 3.89 (3H, s), 4.09 (2×1/6H, d, J=16 Hz), 4.29 (2×1/3H, d, J=15Hz), 4.39 (2×1/3H, d, J=15 Hz), 4.53 (2×1/6H, d, J=16 Hz), 5.08-5.29(1H, m), 6.68 (1×1/4H, d, J=8 Hz), 6.69 (1×3/4H, d, J=8 Hz), 7.10-7.30(5H, m), 7.38 (1H, d, J=8 Hz), 7.90 (1H, s), 7.91 (1×1/4H, s), 7.98(1×3/4H, s)

(40) MASS: 457 (M+1); NMR (CDCl₃, δ): 2.72 (3×3/4H, s), 2.87 (3×1/4H,s), 2.89-3.12 (4H, m), 3.50-3.70 (1H, m), 4.40 (2×1/6H, d, J=16 Hz),4.60 (2×1/6H, d, J=16 Hz), 4.62 (2×1/3H, d, J=15 Hz), 4.68 (2×1/3H, d,J=15 Hz), 5.05-5.30 (1H, m), 6.81 (1H, s), 7.03-7.23 (5H, m), 7.48-7.60(2H, m), 7.67-7.81 (2H, m), 7.91 (1H, s), 8.00-8.20 (2H, m), 8.68(1×1/4H, s), 8.72 (1×3/4H, s)

(41) MASS: 484 (M+1); NMR (CDCl₃, δ): 2.77 (3×2/3H, s), 2.87 (3×1/3H,s), 2.81-3.20 (4H, m), 3.58-3.70 (1H, m), 4.30 (2×1/6H, d, J=16 Hz),4.48 (2×1/6H, d, J=16 Hz), 4.51 (2×1/3H, d, J=15 Hz), 4.58 (2×1/3H, d,J=15 Hz), 5.08-5.22 (1H, m), 6.78-6.88 (1H, m), 7.10-7.31 (5H, m),7.33-7.46 (1H, m), 7.49-7.60 (2H, m), 7.61-7.70 (1H, m), 8.00-8.10 (1H,m), 8.23-8.33 (1H, m), 8.41 (1×1/4H, s), 8.51 (1×3/4H, s), 8.65 (1H, s),9.17 (1H, s)

(42) MASS: 446 (M+1); NMR (CDCl₃, δ): 2.38-2.60 (1H, m), 2.69 (3×2/3H,s), 2.83 (3×1/3H, s), 2.90-3.15 (3H, m), 3.40-3.60 (1H, m), 3.78 (3H,s), 4.31 (2×1/6H, d, J=16 Hz), 4.32 (2×1/3H, d, J=15 Hz), 4.41 (2×1/6H,d, J=16 Hz), 4.69 (2×1/3H, d, J=15 Hz), 5.13-5.26 (1H, m), 6.80-6.90(2H, m), 6.95-7.32 (12H, m), 7.90 (1×1/3H, d, J=8 Hz), 7.99 (1×2/3H, d,J=8 Hz)

(43) MASS: 469 (M+1); NMR (CDCl₃, δ): 2.77 (3×2/3H, s), 2.90 (3×1/3H,s), 2.82-3.12 (3H, m), 3.14-3.31 (1H, m), 3.65-3.72 (1×1/3H, m),3.78-3.85 (1×2/3H, m), 4.52 (2×1/6H, d, J=16 Hz), 4.61 (2×1/6H, d, J=16Hz), 4.62 (2×1/3H, d, J=15 Hz), 4.80 (2×1/3H, d, J=15 Hz), 5.16-5.28(1H, m), 7.10-7.33 (7H, m), 7.43 (1H, d, J=8 Hz), 7.53-7.65 (1H, m),7.77 (1×1/3H, s), 7.83 (1×2/3H, s), 8.01 (1H, d, J=8 Hz), 8.23 (1H, t,J=8 Hz), 8.49-8.58 (1H, m), 8.83 (2H, s)

(44) MASS: 466 (M+1); NMR (CDCl₃, δ): 2.53-2.81 (1H, m), 2.78 (3×2/3H,s), 2.89 (3×1/3H, s), 2.93-3.13 (2H, m), 3.62-3.90 (2H, m), 4.30(2×1/3H, d, J=15 Hz), 4.41 (2×1/3H, s), 4.71 (2×1/3H, d, J=15 Hz),5.20-5.29 (1H, m), 7.00-7.10 (2H, m), 7.12-7.33 (9H, m), 7.36-7.43 (1H,m), 7.45-7.60 (2H, m), 7.77 (1H, d, J=8 Hz), 7.85 (1H, d, J=8 Hz),7.98-8.22 (2H, m)

(45) MASS: 407 (M+1); NMR (CDCl₃, δ): 2.70 (3×3/4H, s), 2.81 (3×1/4H,s), 2.78-3.10 (4H, m), 3.47-3.65 (1H, m), 4.22 (2×1/8H, d, J=16 Hz),4.41 (2×3/8H, d, J=15 Hz), 4.52 (2×3/8H, d, J=15 Hz), 4.63 (2×1/8H, d,J=16 Hz), 5.07-5.20 (1H, m), 6.72-6.85 (1H, m), 7.09-7.31 (6H, m), 7.41(1H, d, J=7 Hz), 7.47-7.60 (1H, m), 7.97-8.05 (1H, m), 8.31 (1×1/4H, s),8.39 (1×3/4H, s), 8.43 (1×1/4H, s), 8.51 (1×3/4H, s)

(46) MASS: 432 (M+1); NMR (CDCl₃, δ): 2.52 (3H, s), 2.67 (3×3/4H, s),2.78 (3×1/4H, s), 2.80-3.10 (3H, m), 3.18-3.30 (1H, m), 3.68-3.80 (1H,m), 4.19 (2×1/8H, d, J=16 Hz), 4.28 (2×3/8H, d, J=15 Hz), 4.33 (2×1/8H,d, J=16 Hz), 4.58 (2×3/8H, d, J=15 Hz), 5.09-5.22 (1H, m), 6.99-7.30(9H, m), 7.61 (1H, t, J=8 Hz), 8.19 (1H, s), 8.21 (1×1/4H, s), 8.29(1×3/4H, s), 8.49-8.53 (1H, m)

(47) MASS: 417 (M+1); NMR (CDCl₃, δ): 2.49-2.73 (1H, m), 2.70 (3×2/3H,s), 2.89 (3×1/3H, s), 2.91-3.22 (3H, m), 3.48-3.53 (1×1/3H, m),3.55-3.63 (1×2/3H, m), 4.31 (2×1/6H, d, J=16 Hz), 4.33 (2×1/3H, d, J=15Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.68 (2×1/3H, d, J=15 Hz), 5.12-5.26(1H, m), 6.98-7.35 (11H, m), 7.48 (1×1/3H, d, J=8 Hz), 7.52 (1×2/3H, d,J=8 Hz), 7.88 (1×1/3H, d, J=8 Hz), 7.92 (1×2/3H, d, J=8 Hz), 8.42(1×1/3H, s), 8.48 (1×2/3H, s), 8.50 (1H, s)

(48) MASS: 450 (M+1); NMR (CDCl₃, δ): 2.43-2.68 (1H, m), 2.69 (3×2/3H,s), 2.88 (3×1/3H, s), 2.90-3.18 (3H, m), 3.42-3.50 (1×1/3H, m),3.52-3.60 (1×2/3H, m), 4.31 (2×1/6H, d, J=16 Hz), 4.32 (2×1/3H, d, J=15Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.69 (2×1/3H, d, J=15 Hz), 5.12-5.23(1H, m), 6.97-7.43 (14H, m), 7.87 (1×1/3H, d, J=8 Hz), 7.94 (1×2/3H, d,J=8 Hz)

(49) MASS: 428 (M+1); NMR (CDCl₃, δ): 2.52-2.78 (1H, m), 2.69 (3×2/3H,s), 2.70-3.12 (3H, m), 2.89 (3×1/3H, s), 3.38-3.49 (1×1/3H, m),4.49-3.58 (1×2/3H, m), 3.80-4.04 (2H, m), 4.33 (2×1/3H, d, J=15 Hz),4.41 (2×1/3H, s), 4.69 (2×1/3H, d, J=15 Hz), 5.14-5.27 (1H, m),6.93-7.33 (14H, m), 7.87 (1×1/3H, d, J=8 Hz), 7.93 (1×2/3H, d, J=8 Hz)

Preparation 62

The following object compounds were obtained by reacting each Startingcompound with di-tert-butyl-dicarbonate in a conventional manner.

(1) MASS: 236 (M+1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.14 (3H, s),2.93-3.03 (2H, m), 4.48-4.58 (1H, m), 5.41 (1H, br s)

(2) mp: 50-53° C.; MASS: 222 (M+1); NMR (CDCl₃, δ): 1.46 (9H, s), 2.32(3H, s), 4.31 (2H, d, J=6 Hz), 4.68 (1H, br s), 7.12-7.27 (4H, m)

(3) MASS: 222 (M+1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.33 (3H, s), 4.28(2H, d, J=8 Hz), 4.72 (1H, br s), 7.07 (2H, d, J=8 Hz), 7.09 (1H, s),7.23 (1H, dd, J=15, 8 Hz)

Preparation 63

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS: 419 (M+1); NMR (CDCl₃, δ): 1.38 (9×1/3H, s), 1.42 (9×2/3H, s),2.60 (3×2/3H, s), 2.81 (3×1/3H, s), 3.07-3.22 (2H, m), 4.14 (2×1/6H, d,J=16 Hz), 4.32 (2×1/6H, d, J=16 Hz), 4.36 (2×1/3H, d, J=15 Hz), 4.59(2×1/3H, d, J=15 Hz), 4.92-5.06 (1H, m), 5.37 (1×1/3H, d, J=10 Hz), 5.45(1×2/3H, d, J=10 Hz), 6.82 (2×1/3H, d, J=8 Hz), 6.92 (2×2/3H, d, J=8Hz), 7.02-7.21 (3H, m), 7.27 (1×1/3H, d, J=8 Hz), 7.32 (1×2/3H, d, J=8Hz), 7.40-7.50 (2H, m), 7.60 (1×1/3H, s), 7.63 (1×2/3H, s), 7.69-7.82(3H, m)

(2) MASS: 383 (M+1); NMR (CDCl₃, δ): 1.08 (9×2/9H, s), 1.19 (9×4/9H, s),1.32 (9×3/9H, s), 2.79-2.93 (6H, m), 2.93-3.29 (2H, m), 4.37-4.75 (2H,m), 4.97-5.08 (1×1/2H, m), 5.30-5.45 (1×1/2H, m), 6.90-7.00 (1H, m),7.03-7.40 (9H, m)

(3) MASS: 399 (M+1); NMR (CDCl₃, δ): 1.38 (9×1/4H, s), 1.40 (9×3/4H, s),2.61 (3×3/4H, s), 2.81 (3×1/4H, s), 2.92 (1H, d, J=8 Hz), 3.77 (3×3/4H,s), 3.79 (3×1/4H, s), 4.17 (2×1/6H, d, J=16 Hz), 4.37 (2×1/6H, d, J=16Hz), 4.40 (2×1/3H, d, J=15 Hz), 4.59 (2×1/3H, d, J=15 Hz), 4.78-4.90(1H, m), 5.31 (1×1/4H, d, J=8 Hz), 5.40 (1×3/4H, d, J=8 Hz), 6.70-6.82(2H, m), 6.92-7.13 (4H, m), 7.20-7.32 (3H, m)

(4) MASS: 383 (M+1); NMR (CDCl₃, δ): 1.39 (9×1/3H, s), 1.41 (9×2/3H, s),2.30 (3×1/3H, s), 2.32 (3×2/3H, s), 2.59 (3×1/3H, s), 2.82 (3×2/3H, s),2.97-3.03 (2H, m), 4.00 (2×1/6H, d, J=16 Hz), 4.37 (2×1/6H, d, J=16 Hz),4.42 (2×1/3H, d, J=15 Hz), 4.49 (2×1/3H, d, J=15 Hz), 4.82-4.97 (1H, m),5.32-5.43 (1H, m), 6.77-7.30 (9H, m)

(5) MPSS 383 (M+1); NMR (CDCl₃, δ): 1.38 (9×1/3H, s), 1.41 (9×2/3H, s),2.13 (3×1/3H, s), 2.22 (3×2/3H, s), 2.63 (3×2/3H, s), 2.87 (3×1/3H, s),2.97-3.08 (2H, m), 3.99 (2×1/6H, d, J=16 Hz), 4.22 (2×1/6H, d, J=16 Hz),4.41 (2×1/3H, d, J=15 Hz), 4.62 (2×1/3H, d, J=15 Hz), 4.70-4.79 (1×1/3H,m), 4.88-4.96 (1×2/3H, m), 5.38 (1H, t, J=8 Hz), 6.78 (1×1/3H, d, J=8Hz), 6.82 (1×2/3H, d, J=8 Hz), 7.05-7.18 (4H, m), 7.22-7.32 (4H, m)

(6) MASS: 371 (M+1); NMR (CDCl₃, δ): 1.38 (9×1/3H, s), 1.40 (9×2/3H, s),2.83 (3×4/5H, s), 2.90 (3×1/5H, s), 2.93-3.12 (2H, m), 4.52 (2×1/2H, d,J=15 Hz), 4.61 (2×1/2H, d, J=15 Hz), 4.89-4.97 (1H, m), 5.29-5.33 (1H,m), 6.80 (1×1/5H, d, J=5 Hz), 6.92 (1×4/5H, d, J=5 Hz), 7.12-7.31 (5H,m), 8.57 (1×1/5H, d, J=5 Hz), 8.59 (1×4/5H, d, J=5 Hz), 9.10 (1H, s)

(7) MASS: 421 (M+1); NMR (CDCl₃, δ): 1.31 (9×1/3H, s), 1.40(9×2/3H, s),2.85 (3×5/6H, s), 2.94 (3×1/6H, s), 2.98-3.15 (2H, m), 4.55 (2×1/6H, d,J=16 Hz), 4.68 (2×1/6H, d, J=16 Hz), 4.73 (2×1/3H, d, J=15 Hz), 4.88(2×1/3H, d, J=15 Hz), 4.88-5.02 (1H, m), 5.32-5.42 (1H, m), 7.10-7.23(5H, m), 7.70-7.80 (2H, m), 7.97-8.03 (1H, m), 8.07-8.13 (1H, m), 8.61(1×1/4H, s), 8.78 (1×3/4H, s)

(8) MASS: 420 (M+1); NMR (CDCl₃, δ): 1.34 (9×1/3H, s), 1.39 (9×2/3H, s),2.80 (3×3/4H, s), 2.92 (3×1/4H, s), 2.98-3.18 (2H, m), 4.51 (2×1/6H, d,J=16 Hz), 4.63 (2×1/6H, d, J=16 Hz), 4.81 (2×2/3H, s), 4.90-5.04 (1H,m), 5.34-5.43 (1H, m), 7.09-7.29 (6H, m), 7.51 (1H, t, J=8 Hz), 7.69(1H, t, J=8 Hz), 7.79 (1H, d, J=8 Hz), 8.01 (1H, d, J=8 Hz), 8.07 (1H,d, J=8 Hz)

(9) MASS: 420 (M+1); NMR (CDCl₃, δ): 1.39 (9×1/4H, s), 1.45 (9×3/4H, s),2.68 (3×3/4H, s), 2.88 (3×1/4H, s), 2.97-3.05 (2H, m), 4.25 (2×1/6H, d,J=16 Hz), 4.58 (2×1/6H, d, J=16 Hz), 4.68 (2×1/3H, d, J=15 Hz), 4.72(2×1/3H, d, J=15 Hz), 4.82-5.00 (1H, m), 5.33-5.47 (1H, m), 7.08-7.32(6H, m), 7.37-7.42 (1H, m), 7.70-7.80 (1H, m), 7.88 (1H, s), 8.13 (1H,d, J=8 Hz), 8.88-8.92 (1H, m)

(10) MASS: 371(M+1); NMR (CDCl₃, δ): 1.40 (9×1/3H, s), 1.42 (9×2/3H, s),2.81 (3×5/6H, s), 2.90 (3×1/6H, s), 2.93-3.08 (2H, m), 4.38 (2×1/6H, d,J=16 Hz), 4.44 (2×1/6H, d, J=16 Hz), 4.58 (2×1/3H, d, J=15 Hz), 4.68(2×1/3H, d, J=15 Hz), 4.83-4.93 (1H, m), 5.29-5.40 (1H, m), 7.13-7.28(5H, m), 8.43-8.50 (3H, m)

(11) MASS: 447 (M+1); NMR (CDCl₃, δ): 1.40 (9×1/4H, s), 1.41 (9×3/4H,s), 2.68 (3×3/4H, s), 2.83 (3×1/4H, s), 2.92-3.12 (2H, m), 4.16 (2×1/6H,d, J=16 Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.53 (2×2/3H, s), 4.82-4.98 (1H,m), 5.32-5.42 (1H, m), 7.12-7.30 (5H, m), 7.38-7.42 (1H, m), 7.48-7.52(1H, m), 7.62 (1×1/4H, d, J=8 Hz), 7.68 (1×3/4H, d, J=8 Hz), 8.25-8.32(1H, m), 8.40 (1×1/4H, s), 8.51 (1×3/4H, s), 8.63 (1H, d, J=5 Hz),9.12-9.20 (1H, m)

(12) MASS: 447 (M+1); NMR (CDCl₃, δ): 1.40 (9×1/4H, s), 1.42 (9×3/4H,s), 2.63 (3×1/4H, s), 2.80 (3×3/4H, s), 2.93-3.10 (2H, m), 4.13 (2×1/6H,d, J=16 Hz), 4.42 (2×1/6H, d, J=16 Hz), 4.49 (2×1/3H, d, J=15 Hz), 4.62(2×1/3H, d, J=15 Hz), 4.82-4.99 (1H, m), 5.32-5.41 (1H, m), 7.15-7.23(4H, m), 7.27-7.32 (2H, m), 7.52 (1H, d, J=8 Hz), 7.70-7.76 (1H, m),8.25-8.40 (2H, m), 8.49 (1H, s), 8.68 (1H, d, J=5 Hz)

(13) MASS (m/z): 321 (M⁺ +1); NMR (CDCl₃, δ): 0.89-1.00 (6H, m), 1.43(9H, s), 1.97 (1H, m), 2.90 (3H×1/3, s), 3.02 (3H×2/3, s), 4.47 (1H×2/3,d, J=15 Hz), 4.50 (1H×1/3, d, J=16 Hz), 4.53 (1H, m), 4.70 (1H×1/3, d,J=16 Hz), 4.74 (1H×2/3, d, J=15 Hz), 5.32 (1H, m), 7.21-7.34 (5H, m)

(14) MASS (m/z): 375 (M⁺ +1); NMR (CDCl₃, δ): 0.85-2.00 (13H, m), 1.45(9H, s), 2.92 (3H×1/3, s), 2.98 (3H×2/3, s), 4.48 (1H×2/3, d, J=15 Hz),4.65 (1H×2/3, d, J=15 Hz), 4.72 (2H×1/3, s), 4.74 (1H, m), 5.17 (1H×1/3,d, J=7 Hz), 5.24 (1H×2/3, d, J=7 Hz), 7.20-7.37 (5H, m)

(15) MASS (m/z): 467 (M⁺ +1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.34 (3H,s), 2.55 (4H, m), 2.58 (3H, s), 2.97 (2H, d, J=7 Hz), 3.18 (4H, m), 3.98(1H×1/3, d, J=16 Hz), 4.30 (1H×1/3, d, J=16 Hz), 4.36 (1H×2/3, d, J=15Hz), 4.45 (1H×2/3, d, J=15 Hz), 4.83 (1H×2/3, q, J=7 Hz), 4.94 (1H×1/3,q, J=7 Hz), 5.37 (1H×1/3, d, J=7 Hz), 5.42 (1H×2/3, d, J=7 Hz),6.79-6.90 (3H, m), 7.02 (1H, d, J=8 Hz), 7.13-7.24 (5H, m)

(16) MASS (m/z): 370 (M⁺ +1); NMR (CDCl₃, δ): 1.37 (9H×1/3s), 1.41(9H×2/3, s), 2.77 (3H×2/3, s), 2.91 (3H×1/3, s), 2.88-3.06 (2H, m), 4.40(1H×4/5, d, J=15 Hz), 4.42 (2H×1/5, s), 4.63 (1H×4/5, d, J=15 Hz), 4.90(1H, m), 5.28 (1H×1/3, d, J=8 Hz), 5.39 (1H×2/3, d, J=8 Hz), 7.02-7.12(4H, m), 7.27-7.32 (3H, m), 8.45 (2H×4/5, d, J=6 Hz), 8.52 (2H×1/5, d,J=6 Hz)

(17) MASS (m/z): 420 (M+H)⁺ ; NMR (CDCl₃, δ): 1.39 (1/5×9H, s), 1.45(4/5×9H, s), 2.68 (4/5×3H, s), 2.86 (1/5×3H, s), 2.92-3.08 (2H, m), 4.22(1/5×1H, d, J=17 Hz), 4.58 (1/5×1H, d, J=17 Hz), 4.68 (4/5×2H, ABq,Δ=0.09, J=15 Hz), 4.80-5.05 (1H, m), 5.30-5.47 (1H, m), 7.06-7.26 (5H,m), 7.50-8.15 (5H, m), 8.62 (1/5×1H, s), 8.76 (4/5×1H, s)

(18) MASS (m/z): 420 (M+H)⁺ ; NMR (CDCl₃, δ): 1.38 (1/4×9H, s), 1.43(3/4×9H, s), 2.68 (3/4×3H, s), 2.88 (1/4×3H, s), 2.92-3.12 (2H, m), 4.40(1/4×2H, ABq, Δ=0.24, J=17 Hz), 4.68 (3/4×2H, ABq, Δ=0.08, J=15 Hz),4.83-5.02 (1H, m), 5.28-5.48 (1H, m), 7.08-7.62 (8H, m), 7.96-8.15 (2H,m), 8.90 (1H, d, J=2 Hz)

(19) MASS (m/z): 427 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 2.21 (3H,s), 2.62 (4/5×3H, s), 2.76 (1/5×3H, s), 2.89-3.08 (2H, m), 3.99 (1/5×1H,d, J=17 Hz), 4.32 (1/5×1H, d, J=17 Hz), 4.43 (4/5×2H, ABq, Δ=0.15, J=15Hz), 4.77-5.00 (1H, m), 5.51 (1H, br d), 7.06-7.48 (6H, m), 7.92-8.28(3H, m)

(20) MASS (m/z): 449 (M+H)⁺ ; NMR (CDCl₃, δ): 1.39 (1/3×9H, s), 1.43(2/3×9H, s), 2.61 (2/3×3H, s), 2.82 (1/3×3H, s), 2.90-3.08 (2H, m), 3.95(3H, s), J=4.11 (1/3×1H, d, =17 Hz), 4.39 (1/3×1H, d, J=17 Hz), 4.51(2/3×2H, ABq, Δ=0.19, J=15 Hz), 4.78-5.02 (1H, m), 5.30-5.50 (1H, m),6.51 (1H, m), 6.93-7.32 (7H, m), 7.38 (1H, s), 7.62-7.78 (2H, m)

(21) MASS (m/z): 413 (M+H)⁺ ; NMR (CDCl₃, δ): 1.41 (9H, s), 2.56(3/4×3H, s), 2.74 (1/4×3H, s), 2.88-3.04 (2H, m), 3.05 (1/4×6H, s), 3.07(3/4×6H, s), 3.79 (1/4×1H, d, J=17 Hz), 4.26 (1/4×1H, d, J=17 Hz), 4.32(3/4×2H, ABq, Δ=0.06, J=15 Hz), 4.72-5.05 (1H, m), 5.31-5.45 (1H, m),6.40 (1/4×1H, d, J=9 Hz), 6.45 (3/4×1H, d, J=9 Hz), 7.00-7.33 (6H, m),7.86 (1/4×1H, d, J=2 Hz), 7.97 (3/4×1H, d, J=2 Hz)

(22) MASS (m/z): 435 (M+H)⁺ ; NMR (CDCl₃, δ): 1.38 (1/4×9H, s), 1.42(3/4×9H, s), 2.67 (3/4×3H, s), 2.83 (1/4×3H, s), 2.91-3.11 (2H, m), 4.25(1/4×2H, ABq, Δ=0.22, J=17 Hz), 4.52 (3/4×2H, ABq, Δ=0.06, J=15 Hz),4.81-4.96 (1H, m), 5.28-5.44 (1H, m), 6.98-7.35 (11H, m), 7.80 (1/4×1H,s), 7.82 (3/4×1H, s)

(23) MASS (m/z): 437 (M+H)⁺ ; NMR (CDCl₃, δ): 1.39 (1/4×9H, s), 1.42(3/4×9H, s), 2.58 (3/4×3H, s), 2.60 (3H, s), 2.81 (1/4×3H, s), 2.88-3.07(2H, m), 3.71 (3H, s), 4.12 (1/4×1H, d, J=17 Hz), 4.52 (1/4×1H, d, J=17Hz), 4.60 (3/4×2H, s), 4.75-5.08 (1H, m), 5.34-5.52 (1H, m), 6.82-7.50(8H, m)

(24) MASS (m/z): 359 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (1/4×9H, s), 1.43(3/4×9H, s), 2.68-2.95 (2H, m), 2.88 (3/4×3H, s), 2.90 (1/4×3H, s), 4.48(1/4×2H, ABq, Δ=0.10, J=17 Hz), 4.56 (3/4×2H, ABq, Δ=0.15, J=15 Hz),4.75-4.90 (1H, m), 5.23-5.43 (1H, m), 6.21 (1/4×1H, s), 6.28 (3/4×1H,s), 7.05-7.40 (7H, m)

(25) MASS (m/z): 373 (M+H)⁺ ; NMR (CDCl₃, δ): 1.41 (9H, s), 2.62(3/4×3H, s), 2.81 (1/4×3H, s), 2.88-3.10 (2H, m), 3.80 (1/4×3H, s), 3.86(3/4×3H, s), 3.90 (1/4×1H, d, J=17 Hz), 4.17 (1/4X 1H, d, J=17 Hz), 4.30(3/4×2H, ABq, Δ=0.11, J=15 Hz), 4.70-5.02 (1H, m), 5.28-5.42 (1H, m),7.02-7.35 (7H, m)

(26) MASS (m/z): 403 (M+H)⁺ ; NMR (CDCl₃, δ): 1.38 (1/3×9H, s), 1.41(2/3×9H, s), 2.71 (2/3×3H, s), 2.81-3.17 (2H, m), 2.87 (1/3×3H, s), 4.36(1/3×2H, ABq, Δ=0.02, J=17 Hz), 4.50 (2/3×2H, ABq, Δ=0.24, J=15 Hz),4.84 (1H, q, J=8 Hz), 5.31 (1/3×1H, d, J=8 Hz), 5.42 (2/3×1H, d, J=8Hz), 6.90-7.85 (9H, m)

(27) MASS (m/z): 359 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (1/4×9H, s), 1.42(3/4×9H, s), 2.80 (3/4×3H, s), 2.88 (1/4×3H, s), 2.90-3.12 (2H, m), 4.41(3/4×1H, d, J=15 Hz), 4.43 (1/4×2H, ABq, Δ=0.19, J=17 Hz), 4.68 (3/4×1H,d, J=15 Hz), 4.87-5.06 (1H, m), 5.30-5.51 (1H, m), 6.08 (1H, s), 6.23(3/4×1H, s), 6.28 (1/4×1H, s), 7.05-7.40 (6H, m)

(28) MASS: 421 (M+1); NMR (CDCl₃, δ): 1.33 (9×1/3H, s), 1.40 (9×2/3H,s), 2.69 (3×2/3H, s), 2.89 (3×1/3H, s), 3.02 (2H, d, J=8 Hz), 4.31(2×1/6H, d, J=16 Hz), 4.58 (2×1/6H, d, J=16 Hz), 4.70 (2×2/3H, s),4.84-4.98 (1H, m), 5.32-5.46 (1H, m), 7.10-7.32 (5H, m), 7.47 (1H, d,J=8 Hz), 7.75 (1×1/3H, s), 7.83 (1×2/3H, s), 7.97-8.07 (1H, m), 8.82(2H, s)

(29) MASS: 419 (M+1); NMR (CDCl₃, δ): 1.41 (9×1/3H, s), 1.43 (9×2/3H,s), 2.03 (3×2/3H, s), 2.65 (3×1/3H, s), 3.27-3.41 (1H, m), 3.57-3.72(1H, m), 3.92 (2×1/6H, d, J=16 Hz), 4.24 (2×1/3H, d, J=15 Hz), 4.31(2×1/6H, d, J=16 Hz), 4.37 (2×1/3H, d, J=15 Hz), 5.02-5.16 (1H, m), 5.51(1×1/3H, d, J=8 Hz), 5.60 (1×2/3H, d, J=8 Hz), 6.70-6.79 (2×1/3H, m),6.90-7.00 (2×2/3H, m), 7.10-7.40 (5H, m), 7.41-7.63 (2H, m), 7.68-7.90(2H, m), 8.11 (1×1/3H, d, J=8 Hz), 8.30 (1×2/3H, d, J=8 Hz)

(30) MASS: 370 (M+1); NMR (CDCl₃, δ): 1.32 (9×1/3H, s), 1.38 (9×2/3H,s), 2.78 (3×2/3H, s), 2.82-3.10 (2H, m), 2.89 (3×1/3H, s), 4.38 (2×1/6H,d, J=16 Hz), 4.46 (2×1/6H, d, J=16 Hz), 4.49 (2×1/3H, d, J=15 Hz), 4.52(2×1/3H, d, J=15 Hz), 4.81-4.92 (1H, m), 5.32 (1×1/3H, d, J=8 Hz), 5.42(1×2/3H, d, J=8 Hz), 7.00-7.20 (3H, m), 7.21-7.34 (3H, m), 7.39 (1×1/3H,d, J=8 Hz), 7.44 (1×2/3H, d, J=8 Hz), 8.32 (1×1/3H, s), 8.48 (1×2/3H,s), 8.41-8.50 (1H, m)

(31) MASS: 335 (M+1); NMR (CDCl₃, δ): 0.78-0.98 (3H, m), 1.18-1.40 (4H,m), 1.41 (9×1/3H, s), 1.42 (9×2/3H, s), 1.49-1.78 (2H, m), 2.91 (3×1/3H,s), 2.98 (3×2/3H, s), 4.50 (2×1/3H, d, J=15 Hz), 4.62 (2×1/3H, d, J=15Hz), 4.68 (2×1/3H, d, J=17 Hz), 4.58-4.73 (1H, m), 5.31 (1×1/3H, d, J=8Hz), 5.39 (1×2/3H, d, J=8 Hz), 7.13-7.40 (5H, m)

Preparation 64

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8, 41 or 54.

(1) MASS: 319 (M+1); NMR (CDCl₃, δ): 2.72 (3×2/3H, s), 2.91 (3×1/3H, s),2.89-3.02 (1H, m), 3.12-3.23 (1H, m), 3.99 (1×1/3H, t, J=8 Hz), 4.10(1×2/3H, t, J=8 Hz), 4.22 (2×1/6H, d, J=16 Hz), 4.39 (2×1/6H, d, J=16Hz), 4.42 (2×1/3H, d, J=15 Hz), 4.69 (2×1/3H, d, J=15 Hz), 6.92-7.39(6H, m), 7.40-7.51 (2H, m), 7.59 (1×1/3H, s), 7.68 (1×2/3H, s),7.71-7.85 (3H, m)

(2) MASS: 283 (M+1); NMR (CDCl₃, δ): 2.25 (3×1/3H, s), 2.37 (3×2/3H, s),2.50 (3×2/3H, s), 2.90 (3×1/3H, s), 2.81-2.91 (1H, m), 2.91-3.05 (1H,m), 3.62-3.78 (1H, m), 3.79 (2×1/6H, d, J=16 Hz), 4.21 (2×1/6H, d, J=16Hz), 4.49 (2×1/3H, d, J=15 Hz), 4.59 (2×1/3H, d, J=15 Hz), 6.96 (2×1/3H,d, J=8 Hz), 7.08 (2×2/3H, d, J=8 Hz), 7.13-7.32 (8H, m)

(3) MASS: 299 (M+1); NMR (CDCl₃, δ): 2.68-2.80 (1H, m), 2.71 (3×2/3H,s), 2.88-2.98 (1H, m), 2.91 (3×1/3H, s), 2.76 (3×2/3H, s), 2.78 (3×1/3H,s), 3.81 (1×1/3H, t, J=8 Hz), 3.91 (1×2/3H, t, J=8 Hz), 4.20 (2×1/6H, d,J=16 Hz), 4.39 (2×1/6H, d, J=16 Hz), 4.41 (2×1/3H, d, J=15 Hz), 4.67(2×1/3H, d, J=15 Hz), 6.78 (2H, t, J=8 Hz), 7.00 -7.18 (4H, m),7.22-7.37 (3H, m)

(4) MASS: 283 (M+1); NMR (CDCl₃, δ): 2.32 (3H, s), 2.69 (3×2/3H, s),2.72-2.81 (1H, m), 2.90 (3×1/3H, s), 2.93-3.03 (1H, m), 3.86-4.00 (1H,m), 4.12 (2×1/4H, d, J=16 Hz), 4.37 (2×1/4H, d, J=16 Hz), 4.46 (2×1/4H,d, J=15 Hz), 4.59 (2×1/4H, d, J=15 Hz), 6.82-7.31 (9H, m)

(5) MASS: 283 (M+1); NMR (CDCl₃, δ): 2.13 (3×1/3H, s), 2.27 (3×2/3H, s),2.72 (3×2/3H, s), 2.78-2.85 (1H, m), 2.97 (3×1/3H, s), 2.98-3.08 (1H,m), 3.70 (1×1/2H, t, J=8 Hz), 4.02 (1×1/2H, t, J=8 Hz), 4.03 (2×1/4H, d,J=16 Hz), 4.73 (2×1/4H, d, J=16 Hz), 4.55 (2×1/4H, d, J=15 Hz), 4.63(2×1/4H, d, J=15 Hz), 6.88-6.93 (1H, m), 7.09-7.18 (4H, m), 7.22-7.32(4H, m)

(6) MASS: 271 (M+1); NMR (CDCl₃, δ): 2.78-2.88 (1H, m), 2.95 (3×2/3H,s), 2.96 (3×1/3H, s), 3.00-3.09 (1H, m), 3.80 (1×1/4H, t, J=7 Hz), 4.05(1×3/4H, t, J=7 Hz), 4.32 (2×1/6H, d, J=17 Hz), 4.42 (2×1/6H, d, J=17Hz), 4.53 (2×1/3H, d, J=15 Hz), 4.69 (2×1/3H, d, J=15 Hz), 6.92 (1×1/4H,d, J=5 Hz), 7.0 (1×3/4H, d, J=5 Hz), 7.12-7.32 (5H, m), 8.62 (1H, d, J=5Hz), 9.11 (1×3/4H, s), 9.13 (1×1/4H, s)

(7) MASS: 321 (M+1); NMR (CDCl₃, δ): 2.78-2.88 (1H, m), 2.90 (3×3/4H,s), 3.00 (3×1/4H, s), 2.98-3.15 (1H, m), 4.02 (1H, t, J=8 Hz), 4.51(2×1/6H, d, J=16 Hz), 4.70 (2×1/6H, d, J=16 Hz), 4.78 (2×1/3H, d, J=15Hz), 4.98 (2×1/3H, d, J=15 Hz), 7.11-7.30 (5H, m), 7.71-7.80 (2H, m),7.98-8.04 (1H, m), 8.08-8.15 (1H, m), 8.66 (1×1/4H, s), 8.82 (1×3/4H, s)

(8) MASS: 320 (M+1); NMR (CDCl₃, δ): 2.79-2.88 (1H, m), 2.85 (3×2/3H,s), 2.97 (3×1/3H, s), 3.02-3.11 (1H, m), 3.98-4.07 (1H, m), 4.51(2×1/6H, d, J=16 Hz), 4.70 (2×1/6H, d, J=16 Hz), 4.80 (2×1/3H, d, J=15Hz), 4.92 (2×1/3H, d, J=15 Hz), 7.11-7.29 (6H, m), 7.51-7.58 (1H, m),7.68-7.73 (1H, m), 7.81 (1H, d, J=8 Hz), 8.01 (1H, d, J=8 Hz), 8.10 (1H,t, J=8 Hz)

(9) MASS: 320 (M+1); NMR (CDCl₃, δ): 2.77 (3×3/4H, s), 2.80-2-88 (1H,m), 2.99 (3×1/4H, s), 3.00-3.09 (1H, m), 3.92-4.05 (1H, m), 4.36(2×1/6H, d, J=16 Hz), 4.59 (2×1/6H, d, J=16 Hz), 4.73 (2×1/3H, d, J=15Hz), 4.80 (2×1/3H, d, J=15 Hz), 7.11-7.31 (5H, m), 7.38-7.42 (2H, m),7.79 (1H, dd, J=8, 2 Hz), 7.85 (1×1/4H, s), 7.89 (1×3/4H, s), 8.15 (1H,d, J=8 Hz), 8.90-8.93 (1H, m)

(10) MASS: 271 (M+1); NMR (CDCl₃, δ): 2.77-2.84 (1H, m), 2.88 (3×3/4H,s), 2.92 (3×1/4H, s), 2.97-3.09 (1H, m), 4.00 (1H, t, J=8 Hz), 4.29(2×1/6, d, J=17 Hz), 4.51 (2×1/6H, d, J=17 Hz), 4.61 (2×1/3H, d, J=15Hz), 4.75 (2×1/3H, d, J=15 Hz), 7.16-7.32 (5H, m), 8.38-8.53 (3H, m)

(11) MASS: 347 (M+1); NMR (CDCl₃, δ): 2.79 (3×4/5H, s), 2.68-2.87 (1H,m), 2.91 (3×1/5H, s), 2.96-3.10 (1H, m), 3.88-4.03 (1H, m), 4.26(2×1/6H, d, J=16 Hz), 4.43 (2×1/6H, d, J=16 Hz), 4.51 (2×1/3H, d, J=15Hz), 4.69 (2×1/3H, d, J=15 Hz), 7.13-7.32 (5H, m), 7.40 (1H, dd, J=8, 5Hz), 7.61 (1H, dd, J=8, 5 Hz), 7.69 (1H, t, J=8 Hz), 8.30 (1H, d, J=8Hz), 8.47 (1×1/5H, s), 8.53 (1×4/5H, s), 8.63 (1H, d, J=5 Hz), 9.18 (1H,s)

(12) MASS: 347 (M+1); NMR (CDCl₃, δ): 2.73 (3×4/5H, s), 2.80-2.90 (1H,m), 2.92 (3×1/5H, s), 2.97-3.09 (1H, m), 3.92-4.02 (1H, m), 4.26(2×1/6H, d, J=16 Hz), 4.45 (2×1/6H, d, J=16 Hz), 4.50 (2×1/3H, d, J=15Hz), 4.74 (2×1/3H, d, J=15 Hz), 7.17-7.42 (6H, m), 7.62 (1H, dd, J=8, 2Hz), 7.82 (1H, t, J=8 Hz), 8.32-8.42 (2H, m), 8.52 (1H, s), 8.70 (1H, d,J=5 Hz)

(13) NMR (CDCl₃, δ): 0.95 (6H×2/3, d, J=7 Hz), 0.99 (6H×1/3, d, J=7 Hz),1.91 (1H, m), 2.94 (3H, s), 3.46 (1H×1/3, d, J=7 Hz), 3.53 (1H×2/3, d,J=7 Hz), 4.43 (1H×1/3, d, J=16 Hz), 4.46 (1H×2/3, d, J=15 Hz), 4.72(1H×1/3, d, J=16 Hz), 4.77 (1H×2/3, d, J=15 Hz), 7.17-7.38 (5H, m)

(14) NMR (CDCl₃, δ): 0.75-1.02 (2H, m), 1.11-1.33 (3H, m), 1.39 (2H, m),1.53-1.88 (6H, m), 2.92 (3H×2/3, s), 2.97 (3H×1/3, s), 3.73 (1H×1/3, dd,J=4, 7 Hz), 3.80 (1H×2/3, dd, J=4, 7 Hz), 4.43 (1H×1/3, d, J=16 Hz),4.48 (1H×2/3, d, J=15 Hz), 4.65 (1H×1/3, d, J=16 Hz), 4.73 (1H×2/3, d,J=15 Hz), 7.16-7.39 (5H, m)

(15) NMR (CDCl₃, δ): 2.35 (3H, s), 2.56 (4H, m), 2.69 (3H×3/5, s), 2.77(1H, dd, J=7, 12 Hz), 2.90 (3H×2/5, s), 2.98 (1H, dd, J=7, 12 Hz), 3.19(4H, m), 3.92 (1H, q, J=7 Hz), 4.07 (1H×2/5, d, J=16 Hz), 4.33 (1H×2/5,d, J=16 Hz), 4.39 (1H×3/5, d, J=15 Hz), 4.52 (1H×3/5, d, J=15 Hz),6.85-6.96 (3H, m), 7.08 (1H, d, J=8 Hz), 7.13-7.31 (5H, m) (16) NMR(CDCl₃, δ): 2.78 (1H, m), 2.80 (3H×3/5, s), 2.97 (3H×2/5, s), 3.00 (1H,m), 3.86 (1H×2/5, t, J=7 Hz), 3.97 (1H×3/5, t, J=7 Hz), 4.37 (1H×2/5, d,J=16 Hz), 4.43 (1H×2/5, d, J=16 Hz), 4.43 (1H×3/5, d, J=15 Hz), 4.68(1H×3/5, d, J=15 Hz), 7.03 (2H, m), 7.15 (2H, m), 7.31 (3H, m), 8.48(2H, m)

(17) MASS (m/z): 320 (M+H)⁺ ; NMR (CDCl₃, δ): 2.72-3.12 (2H, m), 2.77(3/4×3H, s), 2.97 (1/4×3H, s), 3.90-4.07 (1H, m), 4.49 (1/4×2H, ABq,Δ=0.18, J=17 Hz), 4.72 (3/4×2H, ABq, Δ=0.19, J=15 Hz), 7.07-8.17 (10H,m), 8.68 (1/4×1H, s), 8.80 (3/4×1H, s)

(18) MASS (m/z): 320 (M+H)⁺ ; NMR (CDCl₃, δ): 2.76 (3/4×3H, s),2.79-3.10 (2H, m), 2.98 (1/4×3H, s), 3.87-4.08 (1H, m), 4.48 (1/4×2H,ABq, Δ=0.16, J=17 Hz), 4.73 (3/4×2H, ABq, Δ=0.18, J=15 Hz), 7.08-7.65(8H, m), 7.98-8.15 (2H, m), 8.91 (1H, d, J=2 Hz)

(19) MASS (m/z): 327 (M+H)⁺ ; NMR (CDCl₃, δ): 2.21 (3H, s), 2.70(3/4×3H, s), 2.75-3.10 (2H, m), 2.86 (1/4×3H, s), 3.85-4.01 (1H, m),4.22 (1/4×2H, ABq, Δ=0.22, J=17 Hz), 4.49 (3/4×2H, ABq, Δ=0.23, J=15Hz), 7.10-7.55 (6H, m), 7.95-8.20 (3H, m)

(20) MASS (m/z): 275 (M+1)⁺ ; NMR (CDCl₃, δ): 2.86 (3H×2/3, s), 2.96(3H×1/3, s), 2.95-3.05 (1H, m), 3.16-3.29 (1H, m), 3.89 (1H×1/3, t,J=7.0 Hz), 3.97 (1H×2/3, t, J=7.0 Hz), 4.38 (1H×1/3, d, J=14.5 Hz), 4.51(1H, d, J=14.5 Hz), 4.69 (1H×2/3, d, J=14.5 Hz), 6.80 (1H×1/3, d, J=1.5Hz), 6.84 (1H×2/3, d, J=1.5 Hz), 6.89-6.97 (1H, m), 7.09 (1H×2/3, d,J=7.5 Hz), 7.13-7.19 (2H, m), 7.23-7.38 (10/3H, m)

(21) MASS (m/z): 349 (M+H)⁺ ; NMR (CDCl₃, δ): 2.71 (2/3×3H, s),2.73-2.87 (1H, m), 2.92 (1/3×3H, s), 2.95-3.06 (1H, m), 3.84-4.02 (1H,m), 3.93 (3H, s), 4.30 (1/3×2H, ABq, Δ=0.20, J=17 Hz), 4.57 (2/3×2H,ABq, Δ=0.22, J=15 Hz), 6.52 (1H, m), 6.98-7.41 (8H, m), 7.65-7.78 (2H,m)

(22) MASS (m/z): 313 (M⁺ +H); NMR (CDCl₃, δ): 2.68 (3/4×3H, s),2.72-2.82 (1H, m), 2.84 (1/4×3H, s), 2.90-3.03 (1H, m), 3.07 (6H, s),3.88-4.04 (1H, m), 3.99 (1/4×1H, d, J=17 Hz), 4.30 (1/4×1H, d, J=17 Hz),4.40 (3/4×2H, ABq, Δ=0.11, J=15 Hz), 6.43 (1/4×1H, d, J=9 Hz), 6.47(3/4×1H, d, J=9 Hz), 7.06-7.40 (6H, m), 7.92 (1/4×1H, d, J=2 Hz), 7.99(3/4×1H, d, J=2 Hz)

(23) MASS (m/z): 335 (M+H)⁺ ; NMR (CDCl₃, δ): 2.77 (2/3×3H, s),2.77-2.88 (1H, m), 2.92 (1/3×3H, s), 2.96-3.10 (1H, m), 3.82-4.05 (1H,m), 4.33 (1/3×2H, ABq, Δ=0.18, J=17 Hz), 4.58 (2/3×2H, ABq, Δ=0.13, J=17Hz), 7.06-7.37 (11H, m), 7.82 (1H, s)

(24) MASS (m/z): 337 (M+H)⁺ ; NMR (CDCl₃, δ): 2.60 (3H, s), 2.72(3/5×3H, s), 2.73-2.85 (1H, m), 2.92 (2/5×3H, s), 2.93-3.05 (1H, m),3.71 (3H, s), 3.88-4.05 (1H, m), 4.26 (2/5×1H, d, J=17 Hz), 4.54(2/5×1H, d, J=17 Hz), 4.68 (3/5×2H, ABq, Δ=0.01, J=15 Hz), 6.88-7.52(8H, m)

(25) MASS (m/z): 259 (M+H)⁺ ; NMR (CDCl₃, δ): 2.62-2.88 (2H, m), 2.91(2/3×3H, s), 2.97 (1/3×3H, s), 3.79-4.04 (1H, m), 4.33-4.73 (2H, m),6.19 (1/3×1H, s), 6.27 (2/3×1H, s), 7.08-7.41 (7H, m)

(26) MASS (m/z): 273 (M+H)⁺ ; NMR (CDCl₃, δ): 2.69-3.10 (2H, m), 2.72(2/3×3H, s), 2.89 (1/3×3H, s), 3.82 (1/3×3H, s), 3.87 (2/3×3H, s),3.89-4.00 (1H, m), 4.16 (1/3×2H, ABq, Δ=0.15, J=17 Hz), 4.35 (2/3×2H,ABq, Δ=0.12, J=15 Hz), 6.95-7.38 (7H, m)

(27) MASS (m/z): 303 (M+H)⁺ ; NMR (CDCl₃, δ): 2.68-3.04 (2H, m), 2.76(3/5×3H, s), 2.93 (2/5×3H, s), 3.78-4.05 (1H, m), 4.36 (2/5×2H, ABq,Δ=0.11, J=17 Hz), 4.42 (3/5×1H, d, J=15 Hz), 4.68 (3/5×1H, d, J=15 Hz),6.95-7.42 (9H, m)

(28) MASS (m/z): 259 (M+H)⁺ ; NMR (CDCl₃, δ): 2.76-3.08 (2H, m), 2.85(2/3×3H, s), 2.94 (1/3×3H, s), 4.02 (1/3×1H, t, J=7 Hz), 4.08 (2/3×1H,t, J=7 Hz), 4.45 (2/3×1H, d, J=15 Hz), 4.46 (1/3×2H, ABq, Δ=0.19, J=17Hz), 4.72 (2/3×1H, d, J=15 Hz), 6.09 (1H, m), 6.28 (1H, m), 7.08-7.40(6H, m)

(29) MASS: 321 (M+1); NMR (CDCl₃, δ): 2.80 (3×3/4H, s), 2.81-2.91 (1H,m), 3.00 (3×1/4H, s), 3.01-3.11 (1H, m), 3.91 (1×1/4H, t, J=8 Hz), 4.03(1×3/4H, t, J=8 Hz), 4.40 (2×1/6H, d, J=16 Hz), 4.60 (2×1/6H, d, J=16Hz), 4.72 (2×1/3H, d, J=15 Hz), 4.83 (2×1/3H, d, J=15 Hz), 7.10-7.45(5H, m), 7.57 (1H, d, J=8 Hz), 7.82 (1×1/4H, s), 7.88 (1×3/4H, s),8.00-8.10 (1H, m), 8.80-8.88 (2H, m)

(30) MASS: 319 (M+1); NMR (CDCl₃, δ): 2.31 (3×2/3H, s), 2.83 (3×1/3H,s), 3.28-3.47 (2H, m), 3.81 (2×1/6H, d, J=16 Hz), 4.02 (2×1/6H, d, J=16Hz), 4.01-4.09 (1×1/3H, m), 4.13-4.23 (1×2/3H, m), 4.39 (2×1/3H, d, J=15Hz), 4.46 (2×1/3H, d, J=15 Hz), 6.90 (2×1/3H, d, J=8 Hz), 7.03 (2×2/3H,d, J=8 Hz), 7.15-7.60 (7H, m), 7.69-7.80 (1H, m), 7.84 (1H, d, J=8 Hz),7.84 (1×1/3H, d, J=8 Hz), 8.10 (1×2/3H, d, J=8 Hz)

(31) MASS: 270 (M+1); NMR (CDCl₃, δ): 2.70-2.89 (1H, m), 2.78 (3×2/3H,s), 2.90-3.03 (1H, m), 2.99 (3×1/3H, s), 3.82 (1×1/3H, t, J=8 Hz), 3.92(1×2/3H, t, J=8 Hz), 4.32 (2×1/6H, d, J=16 Hz), 4.43 (2×1/6H, d, J=16Hz), 4.49 (2×1/3H, t, J=15 Hz), 4.61 (2×1/3H, d, J=15 Hz), 7.02 (1×2/3H,d, J=7 Hz), 7.19 (1×1/3H, d, J=7 Hz), 7.11-7.40 (5H, m), 7.47 (1×1/3H,d, J=7 Hz), 7.51 (1×2/3H, d, J=7 Hz), 8.37 (1×1/3H, s), 8.47 (1×2/3H,s), 8.48 (1H, s)

(32) MASS: 235 (M+1); NMR (CDCl₃, δ): 0.82-0.95 (3H, m), 1.20-1.55 (5H,m), 1.56-1.73 (1H, m), 2.91 (3×2/3H, s), 2.93 (3×1/3H, s), 3.61-3.75(1H, m), 4.44 (2×1/6H, d, J=16 Hz), 4.50 (2×1/3H, d, J=15 Hz), 4.66(2×1/6H, d, J=16 Hz), 4.70 (2×1/3H, d, J=15 Hz), 7.10-7.40 (5H, m)

Preparation 65

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS: 603 (M+1); NMR (CDCl₃, δ): 1.45 (9H, s), 2-47-3.60 (1H, m),2.51 (3×2/3H, s), 2.79 (3×1/3H, s), 3.08-3.31 (3H, m), 3.36-3.50 (2H,m), 3.50-3.60 (2H, m), 3.61-3.77 (4H, m), 4.18 (2×1/3H, d, J=15 Hz),4.21 (2×1/6H, d, J=16 Hz), 4.28 (2×1/6H, d, J=16 Hz), 4.69 (2×1/3H, d,J=15 Hz), 4.49-4.60 (1H, m), 5.20-5.30 (1H, m), 5.96-6.05 (1H, m), 6.72(2×1/3H, d, J=8 Hz), 6.88 (2×2/3H, d, J=8 Hz), 6.99-7.19 (3H, m),7.28-7.55 (4H, m), 7.61-7.82 (4H, m)

(2) MASS: 567 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.67-2.83 (1H, m),2.79 (3×2/3H, s), 2.89 (3×1/3H, s), 2.92-3.07 (1H, m), 3.10 (3H, s),3.14-3.27 (1H, m), 3.28-3.50 (4H, m), 3.50-3.70 (5H, m), 4.13 (2×1/6H,d, J=16 Hz), 4.20-4.31 (1H, m), 4.37 (2×1/6H, d, J=16 Hz), 4.40 (2×1/3H,d, J=15 Hz), 4.71 (2×1/3H, d, J=15 Hz), 4.80-5.00 (1H, m), 5.64-5.80(1H, m), 6.92 (1H, d, J=5 Hz), 7.10-7.32 (9H, m)

(3) MASS: 583 (M+1); NMR (CDCl₃, δ): 1.48 (9H, s), 2.50-2.62 (1H, m),2.60 (3×2/3H, s), 2.80 (3×1/3H, s), 2.88-3.08 (2H, m), 3.12-3.27 (1H,m), 3.40-3.50 (2H, m), 3.57-3.63 (2H, m), 3.64-3.72 (4H, m), 3.73(3×2/3H, s), 3.79 (3×1/3H, s), 4.18 (2×1/6H, d, J=16 Hz), 4.28 (2×1/3H,d, J=15 Hz), 4.31 (2×1/6H, d, J=16 Hz), 4.50-4.70 (1H, m), 4.68 (2×1/3H,d, J=15 Hz), 5.00-5.14 (1H, m), 5.95-6.07 (1H, m), 6.72 (2×2/3H, d, J=8Hz), 6.80 (2×1/3H, d, J=8 Hz), 6.83-6.92 (1H, m)

(4) MASS: 526 (M+1); NMR (CDCl₃, δ): 1.48 (9H, s), 2.51-2.62 (1H, m),2.52 (3H, s), 2.53 (3×2/3H, s), 2.73 (3×1/3H, s), 2.94 (3H, s),2.98-3.03 (2H, m), 3.01 (3H, s), 3.09-3.30 (1H, m), 4.00 (2×1/6H, d,J=17 Hz), 4.22 (2×1/6H, d, J=17 Hz), 4.27 (2×1/3H, d, J=15 Hz), 4.54(2×1/3H, d, J=15 Hz), 4.50-4.58 (1H, m), 5.06-5.18 (1H, m), 6.08-6.14(1H, m), 6.92-7.30 (7H, m), 7.51 (1H, t, J=8 Hz), 8.14 (1×1/4H, s), 8.28(1×3/4H, s)

(5) MASS: 580 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.27 (3×1/3H, s),2.31 (3×2/3H, s), 2.29 (3H, s), 2.32-2.44 (4H, m), 2.49-2.61 (1H, m),2.50 (3×2/3H, s), 2.80 (3×1/3H, s), 2.97-3.11 (2H, m), 3.17-3.28 (1H,m), 3.40-3.50 (2H, m), 3.57-3.65 (2H, m), 4.02 (2×1/6H, d, J=16 Hz),4.23 (2×1/6H, d, J=16 Hz), 4.28 (2×1/3H, d, J=15 Hz), 4.58 (2×1/3H, d,J=15 Hz), 4.48-4.56 (1H, m), 5.08-5.18 (1H, m), 5.99-6.07 (1H, m),6.66-7.47 (10H, m)

(6) MASS: 580 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.17 (3×2/3H, s),2.28 (3×1/3H, s), 2.28 (3H, s), 2.32-2.42 (4H, m), 2.48-2.61 (1H, m),2.54 (3×2/3H, s), 2.80 (3×1/3H, s), 2.95-3.28 (3H, m), 3.40-3.50 (2H,m), 3.55-3.65 (2H, m), 4.00 (2×1/4H, d, J=16 Hz), 4.13 (2×1/4H, d, J=16Hz), 4.49 (2×1/2H, s), 4.50-4.59 (1H, m), 4.93-5.02 (1×1/3H, m),5.13-5.21 (1×2/3H, m), 6.00 (1H, d, J=8 Hz), 6.63 (1×1/3H, d, J=8 Hz),6.71 (1×2/3H, d, J=8 Hz), 7.02-7.18 (4H, m), 7.20-7.30 (4H, m),7.38-7.45 (1H, m)

(7) MASS: 555 (M+1); NMR (CDCl₃, δ): 1.47 (9×3/4H, s), 1.48 (9×1/4H, s),2.51-2.62 (1H, m), 2.81 (3×3/4H, s), 2.88 (3×1/4H, s), 2.94-3.23 (3H,m), 3.43-3.49 (2H, m), 3.57-3.62 (2H, m), 3.63-3.73 (4H, m), 4.36(2×1/6H, d, J=17 Hz), 4.40 (2×1/6H, d, J=17 Hz), 4.47 (2×1/3H, d, J=15Hz), 4.51-4.60 (1H, m), 4.61 (2×1/3H, d, J=15 Hz), 4.92-5.00 (1×1/4H,m), 5.13-5.22 (1×3/4H, m), 5.97-6.05 (1H, m), 6.72 (1×1/4H, d, J=5 Hz),6.82 (1×3/4H, d, J=5 Hz), 7.18-7.30 (5H, m), 7.33 (1×1/4H, d, J=8 Hz),7.40 (1×3/4H, d, J=8 Hz), 8.54 (1×1/4H, d, J=5 Hz), 8.59 (1×3/4H, d, J=5Hz), 9.08 (1×1/4H, s), 9.10 (1×3/4H, s)

(8) MASS: 605 (M+1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.49-2.62 (1H, m),2.79 (3×5/6H, s), 2.93 (3×1/6H, s), 3.00-3.23 (3H, m), 3.40-3.50 (2H,m), 3.53-3.62 (2H, m), 3.63-3.73 (6H, m), 4.51 (2×1/6H, d, J=16 Hz),4.58 (2×1/6H, d, J=16 Hz), 4.62 (2×1/3H, d, J=15 Hz), 4.92 (2×1/3H, d,J=15 Hz), 4.50-4.63 (1H, m), 7.08-7.21 (5H, m), 7.47-7.53 (1H, m),7.71-7.80 (2H, m), 7.98-8.03 (1H, m), 8.07-8.13 (1H, m), 8.61 (1×1/6H,s), 8.74 (1×5/6H, s)

(9) MASS: 604 (M+1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.49-2.61 (1H, m),2.72 (3×2/3H, s), 2.89 (3×1/3H, s), 3.00-3.25 (3H, m), 3.40-3.50 (2H,m), 3.56-3.62 (2H, m), 3.63-3.73 (4H, m), 4.48 (2×1/6H, d, J=17 Hz),4.58 (2×1/6H, d, J=17 Hz), 4.50-4.61 (1H, m), 4.69 (2×1/3H, d, J=15 Hz),4.85 (2×1/3H, d, J=15 Hz), 5.17-5.28 (1H, m), 5.97-6.04 (1H, m), 7.03(1×1/4H, d, J=8 Hz), 7.09 (1×3/4H, d, J=8 Hz), 7.18-7.24 (5H, m),7.41-7.56 (2H, m), 7.70 (1H, t, J=8 Hz), 7.80 (1H, d, J=8 Hz), 7.97-8.08(2H, m)

(10) MASS: 604 (M+1); NMR (CDCl₃, δ): 1.49 (9H, s), 2.52-2.60 (1H, m),2.62 (3×2/3H, s), 2.83 (3×1/3H, s), 2.99-3.27 (3H, m), 3.40-3.50 (2H,m), 3.58-3.62 (2H, m), 3.64-3.74 (4H, m), 4.21 (2×1/6H, d, J=16 Hz),4.50 (2×1/6H, d, J=16 Hz), 4.53-4.62 (1H, m), 4.60 (2×1/3H, d, J=15 Hz),4.73 (2×1/3H, d, J=15 Hz), 5.11-5.27 (1H, m), 5.97-6.08 (1H, m),7.02-7.30 (6H, m), 7.40 (1H, dd, J=8, 5 Hz), 7.44-7.53 (1H, m),7.70-7.80 (1H, m), 7.83 (1H, s), 8.14 (1H, t, J=5 Hz), 8.89 (1H, t, J=5Hz)

(11) MASS: 555 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.52-2.60 (1H, m),2.78 (3×3/4H, s), 2.88 (3×1/4H, s), 3.02-3.22 (2H, m), 3.41-3.50 (2H,m), 3.57-3.72 (7H, m), 4.36 (2×1/3H, s), 4.47 (2×1/3H, d, J=15 Hz),4.48-4.60 (1H, m), 4.70 (2×1/3H, d, J=15 Hz), 5.08-5.16 (1H, m), 6.00(1H, br s), 7.13-7.28 (6H, m), 7.47 (1H, br s), 8.41-8.50 (2H, m)

(12) MASS: 631 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.51-2.62 (1H, m),2.62 (3×3/4H, s), 2.80 (3×1/4H, s), 2.98-3.28 (3H, m), 3.40-3.52 (2H,m), 3.55-3.62 (2H, m), 3.62-3.72 (4H, m), 4.14 (2×1/6H, d, J=16 Hz),4.32 (2×1/6H, d, J=16 Hz), 4.40 (2×1/3H, d, J=15 Hz), 4.51-4.60 (1H, m),4.61 (2×1/3H, d, J=15 Hz), 5.08-5.20 (1H, m), 5.99-6.06 (1H, m),7.12-7.30 (5H, m), 7.38-7.50 (3H, m), 7.59 (1×1/4H, d, J=8 Hz), 7.67(1×3/4H, d, J=8 Hz), 8.26-8.32 (1H, m), 8.33 (1×1/4H, s), 8.48 (1×3/4H,s), 8.64 (1H, d, J=5 Hz), 9.12-9.20 (1H, m)

(13) MASS: 631 (M+1); NMR (CDCl₃, δ): 1.43 (9H, s), 2.52-2.62 (1H, m),2.59 (3×3/4H, s), 2.80 (3×1/4H, s), 2.99-3.22 (3H, m), 3.42-3.50 (2H,m), 3.58-3.62 (2H, m), 3.67-3.77 (4H, m), 4.18 (2×1/6H, d, J=16 Hz),4.32 (2×1/6H, d, J=16 Hz), 4.31 (2×1/3H, d, J=15 Hz), 4.71 (2×1/3H, d,J=15 Hz), 4.51-4.60 (1H, m), 5.08-5.22 (1H, m), 6.02 (1H, br s),7.18-7.22 (5H, m), 7.28-7.33 (1H, m), 7.41-7.51 (2H, m), 7.79-7.88 (1H,m), 8.22-8.46 (3H, m), 8.66-8.70 (1H, m)

(14) MASS: 505 (M⁺ +1); NMR (CDCl₃, δ): 0.88-0.99 (6H, m), 1.47 (9H, s),2.07 (1H, m), 2.57 (1H, m), 2.91 (3H×1/3, s), 3.01 (3H×2/3, s), 3.21(1H, dd, J=3, 15 Hz), 3.45 (2H, m), 3.58 (2H, m), 3.65 (4H, m), 4.37(1H×2/3, d, J=15 Hz), 4.57 (1H, m), 4.63 (2H×1/3, s), 4.81 (1H, m), 4.82(1H×2/3, d, J=15 Hz), 6.12 (1H, m), 7.21-7.35 (5H, m)

(15) MASS: 559 (M⁺ +1); NMR (CDCl₃, δ): 0.80-1.00 (2H, m), 1.07-1.25(3H, m), 1.45 (9H, s), 1.43-1.94 (8H, m), 2.55 (1H, m), 2.92 (3H×1/3,s), 2.98 (3H×2/3, s), 3.17 (1H, dd, J=4, 15 Hz), 3.44 (2H, m), 3.60 (2H,m), 3.66 (4H, m), 4.38 (1H×2/3, d, J=15 Hz), 4.56 (1H×1/3, d, J=16 Hz),4.55 (1H, m), 4.67 (1H×1/3, d, J=16 Hz), 4.75 (1H×2/3, d, J=15 Hz), 5.02(1H, m), 6.03 (1H, d, J=7 Hz), 7.17-7.38 (5H, m)

(16) MASS: 651 (M⁺ +1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.35 (3H, s), 2.51(3H×2/3, s), 2.56 (5H, m), 2.74 (3H×1/3, s), 3.02 (2H, m), 3.18 (5H, m),3.45 (2H, m), 3.60 (2H, m), 3.67 (4H, m), 3.92 (1H×1/3, d, J=16 Hz),4.22 (1H×1/3, d, J=16 Hz), 4.23 (1H×2/3, d, J=15 Hz), 4.52 (1H×2/3, d,J=15 Hz), 4.54 (1H, m), 5.07 (1H×2/3, m), 5.17 (1H×1/3, m), 6.00 (1H, d,J=7 Hz), 6.80 (4H×1/3, s), 0.82 (2H×2/3, s), 6.97 (2H×2/3, s), 7.19 (4H,s), 7.44 (1H, m)

(17) MASS (m/z): 554 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.46-2.58(1H, m), 2.72 (3H×2/3, s), 2.88 (3H×1/3, s), 2.90-2.99 (1H, m), 3.08(1H, dd, J=7, 13 Hz), 3.18 (1H, m), 3.43 (2H, m), 3.57 (2H, m), 3.65(4H, m), 4.26 (1H×2/3, d, J=15 Hz), 4.35 (1H×1/3, d, J=16 Hz), 4.44(1H×1/3, d, J=16 Hz), 4.52 (1H, m), 4.70 (1H×2/3, d, J=15 Hz), 5.15 (1H,m), 5.98 (1H, d, J=7 Hz), 6.92-7.13 (4H, m), 7.27-7.45 (3H, m), 8.43(2H, m)

(18) MASS (m/z): 620 (M⁺ +1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.61(3H×3/4, s), 2.80 (3H×1/4, s), 2.95-3.23 (4H, m), 3.45 (2H, m), 3.60(2H, m), 3.67 (4H, m), 4.16 (1H×1/4, d, J=16 Hz), 4.30 (1H×1/4, d, J=16Hz), 4.38 (1H×3/4, d, J=15 Hz), 4.54 (1H, m), 4.63 (1H×3/4, d, J=15 Hz),5.13 (1H, m), 6.02 (1H, m), 6.97-7.17 (2H, m), 7.21-7.28 (4H, m),7.36-7.58 (3H, m), 8.09 (1H, s), 8.52 (1H, s)

(19) MASS (m/z): 604 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.49-2.66(1H, m), 2.61 (3/4×3H, s), 2.83 (1/4×3H, s), 2.94-3.28 (3H, m),3.35-3.76 (8H, m), 4.38 (1/4×2H, ABq, Δ=0.19, J=17 Hz), 4.49 (3/4×1H, d,J=15 Hz), 4.50-4.65 (1H, m), 4.80 (3/4×1H d, J=15 Hz), 5.02-5.25 (1H,m), 5.93-6.10 (1H, br d), 7.03-7.30 (5H, m), 7.40-8.15 (6H, m), 8.58(1/4×1H, d, J=2 Hz), 8.72 (3/4×1H, d, J=2 Hz)

(20) MASS: 604 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.48-2.68 (1H, m),2.62 (2/3×3H, s), 2.84 (1/3×3H, s), 2.94-3.28 (3H, m), 3.37-3.78 (8H,m), 4.38 (1/3×2H, ABq, Δ=0.11, J=17 Hz), 4.49 (2/3×1H, d, J=15 Hz),4.50-4.64 (1H, m), 4.80 (2/3×1H, d, J=15 Hz), 5.10-5.24 (1H, m),5.96-6.08 (1H, br d), 7.10-7.55 (9H, m), 7.93-8.15 (2H, m), 8.86-8.92(1H, m)

(21) MASS (m/z): 611 (M+H)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 2.19(1/4×3H, s), 2.21 (3/4×3H, s), 2.50-2.63 (1H, m), 2.55 (3/4×3H, s), 2.72(1/4×3H, s), 2.93-3.28 (3H, m), 3.37-3.78 (8H, m), 4.11 (1/4×2H, ABq,Δ=0.22, J=17 Hz), 4.21 (3/4×1H, d, J=15 Hz), 4.48-4.60 (1H, m), 4.58(3/4×1H, d, J=15 Hz), 5.02-5.22 (1H, m), 5.95-6.10 (1H, br d), 7.05-7.52(7H, m), 7.86-8.15 (3H, m)

(22) MASS (m/z): 588 (M+H)⁺ ; NMR (CDCl₃, δ): 1.43 (9H, s), 1.8-2.2 (2H,m), 2.3-2.5 (2H, m), 2.60 (2/3×3H, s), 2.82 (1/3×3H, s), 3.0-3.1 (2H,m), 4.10 (1/3×1H, d, J=15 Hz), 4.1-4.2 (1H, m), 4.32 (1/3×1H, d, J=15Hz), 4.38 (2/3×1H, d, J=15 Hz), 4.60 (2/3×1H, d, J=15 Hz), 5.1-5.2 (2H,m), 5.13 (2H, s), 6.9-7.3 (16H, m)

(23) MASS (m/z): 537 (M⁺ +1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.52-3.28(4H, m), 3.42-3.68 (8H, m), 4.52-4.68 (2H, m), 4.89-4.97 (1H, m),5.39-5.47 (1H, m), 6.90 (1H, d, J=8 Hz), 7.01 (1H, t, J=8 Hz), 7.13 (1H,t, J=8 Hz), 7.18-7.34 (6H, m), 6.79-7.85 (1H, m)

(24) MASS (m/z): 559 (M+1)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.49-2.62(1H, m), 2.76 (3H×2/3, s), 2.84 (3H×1/3, s), 3.11-3.26 (2H, m), 3.32(1H×2/3, x, J=8.5 Hz), 3.38 (1H×1/3, d, J=8.5 Hz), 3.40-3.50 (2H, m),3.55-3.76 (6H, m), 4.33 (1H×1/3, d, J=14.5 Hz), 4.37 (1H×2/3, d, J=14.5Hz), 4.41 (1H×1/3, d, J=14.5 Hz), 4.47-4.60 (1H, m), 4.64 (1H×2/3, d,J=14.5 Hz), 5.10-5.19 (1H, m), 6.02 (1H, br d, J=7.5 Hz), 6.83-7.33 (8H,m), 7.40 (1H×1/3, br d, J=7.5 Hz), 7.47 (1H×2/3, br d, J=7.5 Hz)

(25) MASS (m/z): 633 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.47-2.62(1H, m), 2.54 (2/3×3H, s), 2.79 (1/3×3H, s), 2.93-3.11 (2H, m),3.11-3.28 (1H, m), 3.35-3.75 (8H, m), 3.94 (3H, s), 4.20 (1/3×2H, ABq,Δ=0.21, J=17 Hz), 4.26 (2/3×1H, d, J=15 Hz), 4.49-4.62 (1H, m), 4.68(2/3×1H, d, J=15 Hz), 5.05-5.23 (1H, m), 6.02 (1H, br d, J=8 Hz), 6.50(1/3×1H, d, J=2 Hz), 6.52 (2/3×1H, d, J=2 Hz), 6.87-7.73 (11H, m)

(26) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.50(2/3×3H, s), 2.51-2.62 (1H, m), 2.71 (1/3×3H, s), 2.97-3.06 (2H, m),3.06 (1/3×6H, s), 3.08 (2/3×6H, s), 3.11-3.28 (1H, m), 3.36-3.80(8H+1/3×2H, m), 4.31 (2/3×2H, ABq, Δ=0.21, J=15 Hz), 4.47-4.61 (1H, m),4.98-5.32 (1H, m), 6.02 (1H, br d, J=8 Hz), 6.39 (1/3×1H, d, J=9 Hz),6.43 (2/3×1H, d, J=9 Hz), 7.12-7.52 (7H, m), 7.82 (1/3×1H, d, J=2 Hz),7.94 (2/3×tH, d, J=2 Hz)

(27) MASS (m/z): 619 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.49-2.65(1H, m), 2.61 (2/3×3H, s), 2.79 (1/3×3H, s), 2.92-3-30 (3H, m),3.36-3.78 (8H, m), 4.22 (1/3×2H, ABq, Δ=0.15, J=17 Hz), 4.46-4.62 (1H,m), 4.49 (2/3×2H, ABq, Δ=0.16, J=15 Hz), 5.06-5.21 (1H, m), 5.92-6.08(1H, m), 6.92-7.50 (12H, m), 7.82 (1H, s)

(28) MASS (m/z): 621 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 2.48-2.65(1H, m), 2.52 (2/3×3H, s), 2.58 (1/3×3H, s), 2.60 (2/3×3H, s), 2.76(1/3×3H, s), 2.93-3.27 (3H, m), 3.36-3.77 (8H, m), 3.69 (1/3×3H, s),3.71 (2/3×3H, s), 4.02 (1/3×1H, d, J=17 Hz), 4.47 (1/3×1H, d, J=17 Hz),4.48-4.62 (1H, m), 4.57 (2/3×2H, ABq, Δ=0.16, J=15 Hz), 5.02-5.34 (1H,m), 6.02 (1H, br d), 6.75-7.56 (9H, m)

(29) MASS (m/z): 543 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45 (9H, s), 2.46-2.62(1H, m), 2.70-3.02 (2H, m), 2.85 (2/3×3H, s), 2.88 (1/3×3H, s),3.11-3.30 (1H, m), 3.37-3.76 (8H, m), 4.36 (2/3×1H, d, J=15 Hz),4.45-4.60 (1H, m), 4.48 (1/3×2H, s), 4.70 (2/3×1H, d, J=15 Hz),5.00-5.12 (1H, m), 6.02 (1H, br d, J=8 Hz), 6.23 (1/3×1H, s), 6.28(2/3×1H, s), 7.00-7.50 (8H, m)

(30) MASS (m/z): 557 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.50-2.62(1H, m), 2.56 (2/3×3H, s), 2.78 (1/3×3H, s), 2.92-3.28 (3H, m),3.38-3.75 (8H, m), 3.79 (1/3×3H, s), 3.85 (2/3×3H, s), 4.01 (1/3×2H,ABq, Δ=0.16, J=17 Hz), 4.13 (2/3×1H, d, J=15 Hz), 4.40 (2/3×1H, d, J=15Hz), 4.46-4.60 (1H, m), 4.98-5.23 (1H, m), 5.93-6.09 (1H, m), 6.88-7.50(8H, m)

(31) MASS (m/z): 587 (M+H)⁺ ; NMR (CDCl₃, δ): 1.46 (9H, s), 2.45-2.62(1H, m), 2.67 (2/3×3H, s), 2.83 (1/3×3H, s), 2.85-3.27 (3H, m),3.35-3.76 (8H, m), 4.25 (2/3×1H, d, J=15 Hz), 4.34 (1/3×2H, ABq, Δ=0.06,J=17 Hz), 4.45-4.60 (1H, m), 4.71 (2/3×1H, d, J=15 Hz), 5.04-5.16 (1H,m), 6.00 (1H, d, J=8 Hz), 6.84-7.48 (10H, m)

(32) MASS (m/z): 543 (M+H)⁺ ; NMR (CDCl₃, δ): 1.48 (9H, s), 2.48-2.67(1H, m), 2.78 (2/3×3H, s), 2.86 (1/3×3H, s), 2.94-3.28 (3H, m),3.35-3.79 (8H, m), 4.31 (2/3×1H, d, J=15 Hz), 4.41 (1/3×2H, ABq, Δ=0.13,J=17 Hz), 4.46-4.63 (1H, m), 4.77 (2/3×1H, d, J=15 Hz), 5.10-5.30 (1H,m), 5.92-6.10 (1H, br d, J=8 Hz), 6.11 (2/3×1H, d, J=2 Hz), 6.13(1/3×1H, d, J=2 Hz), 6.24 (2/3×1H, d, J=2 Hz), 6.30 (1/3×1H, d, J=2 Hz),7.02-7.60 (7H, m)

(33) MASS: 605 (M+1); NMR (CDCl₃, δ): 1.49 (9H, s), 2.50-2.70 (1H, m),2.63 (3×2/3H, s), 2.83 (3×1/3H, s), 2.97-3.30 (3H, m), 3.40-3.50 (2H,m), 3.58-3.64 (2H, m), 3.65-3.80 (4H, m), 4.32 (2×1/6H, d, J=16 Hz),4.49 (2×1/6H, d, J=16 Hz), 4.51-4.63 (1H, m), 4.59 (2×1/3H, d, J=15 Hz),4.80 (2×1/3H, d, J=15 Hz), 5.10-5.21 (1H, m), 5.95-6.08 (1H, m),7.15-7.28 (5H, m), 7.39-7.53 (2H, m), 7.71 (1×1/3H, s), 7.82 (1×2/3H,s), 7.98 (1×1/3H, d, J=8 Hz), 8.00 (1×2/3H, d, J=8 Hz), 8.82 (2H, s)

(34) MASS: 603 (M+1);

NMR (CDCl₃, δ): 1.49 (9H, s), 1.91 (3×2/3H, s), 2.61 (3×1/3H, s),3.20-3.53 (4H, m), 3.54-3-86 (8H, m), 4.22 (2×1/2H, d, J=15 Hz), 4.36(2×1/2H, d, J=15 Hz), 4.50-4.63 (1H, m), 5.28-5.38 (1H, m), 6.00-6.10(1H, m), 6.61-6.68 (2×1/3H, m), 6.88-7.00 (2×2/3H, m), 7.07-7.30 (5H,m), 7.31-7.72 (4H, m), 7.74-7.86 (1H, m), 8.19 (1×1/3H, d, J=8 Hz), 8.39(1×2/3H, d, J=8 Hz)

(35) MASS: 554 (M+1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.48-2.61 (1H, m),2.71 (3×2/3H, s), 2.88 (3×1/3H, s), 2.89-3.27 (3H, m), 3.35-3.49 (1H,m), 3.52-3.75 (7H, m), 4.38 (2×1/3H, s), 4.39 (2×1/3H, d, J=15 Hz), 4.59(2×1/3H, d, J=15 Hz), 4.44-4.58 (1H, m), 5.07-5.18 (1H, m), 5.96-6.06(1H, m), 6.91-6.98 (2×1/3H, m), 7.08-7.11 (2×2/3H, m), 7.06-7.20 (1H,m), 7.22-7.33 (3H, m), 7.38-7.57 (2H, m), 8.38 (1×1/3H, s), 8.47(1×2/3H, s), 8.47 (1H, s)

(36) MASS: 584 (M+1); NMR (CDCl₃, δ): 1.48 (9H, s), 2.51 (3×3/4H, s),2.71 (3×1/4H, s), 2.49-2.63 (1H, m), 2.95-3.05 (2H, m), 3.06-3.25 (1H,m), 3.38-3.50 (2H, m), 3.53-3.62 (2H, m), 3.62-3.77 (4H, m), 3.88(3×1/4H, s), 3.99 (3×3/4H, s), 4.20 (2×1/2H, d, J=16 Hz), 4.49 (2×1/2H,d, J=16 Hz), 4.50-4.60 (1H, m), 5.00-5.11 (1H, m), 5.95-6.07 (1H, m),6.60-6.70 (1H, m), 7.00 (1×1/4H, d, J=8 Hz), 7.18 (1×3/4H, d, J=8 Hz),7.10-7.30 (5H, m), 7.43 (1H, t, J=8 Hz), 7.80 (1×1/4H, s), 7.92 (1×3/4H,s)

(37) MASS: 519 (M+1); NMR (CDCl₃, δ): 0.78-1.00 (3H, m), 1.15-1.41 (4H,m), 1.47 (9H, s), 1.56-1.71 (2H, m), 2.48-2.62 (1H, m), 2.91 (3×1/3H,s), 2.97 (3×2/3H, s), 3.20 (1H, d, J=16 Hz), 3.35-3.50 (2H, m),3.52-3.60 (2H, m), 3.61-3.78 (4H, m), 4.41 (2×1/3H, d, J=15 Hz),4.49-4.63 (1H, m), 4.61 (2×1/3H, s), 4.77 (2×1/3H, d, J=15 Hz),4.87-5.00 (1H, m), 6.08 (1H, d, J=8 Hz), 7.12-7.50 (6H, m)

Preparation 66

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8, 41 or 54.

(1) MASS: 503 (M+1); NMR (CDCl₃, δ): 1.97-2.03 (1×1/3H, m), 2.20-2.30(1×2/3H, m), 2.47 (1×1/3H, dd, J=15, 2 Hz), 2.60 (1×2/3H, dd, J=15, 2Hz), 2.72 (3×2/3H, s), 2.90 (3×1/3H, s), 2.98-3.33 (4H, m), 3.40-3.72(7H, m), 4.30 (2×1/3H, d, J=15 Hz), 4.42 (2×1/6H, d, J=16 Hz), 4.50(2×1/6H, d, J=16 Hz), 4.71 (2×1/3H, d, J=15 Hz), 5.26-5.38 (1H, m),6.92-7.02 (2H, m), 7.10-7.23 (3H, m), 7.34-7.48 (3H, m), 7.59 (1×1/3H,s), 7.69 (1×2/3H, s), 7.70-7.81 (3H, m), 8.03 (1×1/3H, d, J=8 Hz), 8.19(1×2/3H, d, J=8 Hz)

(2) MASS: 467 (M+1); NMR (CDCl₃, δ): 2.64 (1×2/3H, d, J=8 Hz), 2.71(1×1/3H, d, J=8 Hz), 2.80 (3×2/3H, s), 2.89 (3×1/3H, s), 2.91-3.14 (2H,m), 3.11 (3H, s), 3.15-3.42 (3H, m), 3.43-3.70 (8H, m), 3.93 (1×1/3H, t,J=8 Hz), 4.08 (1×2/3H, t, J=8 Hz), 4.36 (2×1/6H, d, J=16 Hz), 4.47(2×1/3H, d, J=15 Hz), 4.62 (2×1/3H, d, J=15 Hz), 4.68 (2×1/6H, d, J=16Hz), 5.73-5.83 (1H, m), 6.97 (2×1/3H, d, J=7 Hz), 7.13 (2×2/3H, d, J=7Hz), 7.18-7.33 (8H, m)

(3) MASS: 483 (M+1); NMR (CDCl₃, δ): 2.27-2.39 (1×1/3H, m), 2.42-2.53(1×2/3H, m), 2.60-2.82 (1H, m), 2.68 (3×2/3H, s), 2.88 (3×1/3H, s),2.90-3.08 (2H, m), 3.33-3.48 (2H, m), 3.50-3.72 (7H, m), 3.73 (3×2/3H,s), 3.76 (3×1/3H, s), 4.30 (2×1/3H, d, J=15 Hz), 4.40 (2×1/3H, s), 4.71(2×1/3H, d, J=15 Hz), 5.08-5.19 (1H, m), 6.70-6.82 (2H, m), 6.93-7.15(4H, m), 7.20-7.32 (3H, m), 8.01 (1×1/3H, d, J=8 Hz), 8.11 (1×2/3H, d,J=8 Hz)

(4) MASS: 426 (M+1); NMR (CDCl₃, δ): 2.50-2.62 (1H, m), 2.51 (3×1/3H,s), 2.52 (3×2/3H, s), 2.63 (3×2/3H, s), 2.72-2.85 (1H, m), 2.79 (3×1/3H,s), 2.91-3.22 (2H, m), 2.99 (3H, s), 3.00 (3H, s), 3.62-3.80 (1H, m),4.22 (2×1/6H, d, J=17 Hz), 4.32 (2×1/3H, d, J=15 Hz), 4.38 (2×1/6H, d,J=17 Hz), 4.60 (2×1/3H, d, J=17 Hz), 5.10-5.23 (1H, m), 7.01-7.11 (1H,m), 7.14-7.31 (6H, m), 8.18 (1H, m), 8.21 (1×1/4H, s), 8.30 (1×3/4H, s)

(5) MASS: 480 (M+1); NMR (CDCl₃, δ): 2.30 (3H, s), 2.31 (3H, s),2.22-2.48 (5H, m), 2.68 (3×2/3H, s), 2.72-2.85 (1H, m), 2.89 (3×1/3H,s), 2.92-3.16 (2H, m), 3.39-3.48 (2H, m), 3.52-3.73 (3H, m), 4.30(2×1/6H, d, J=16 Hz), 4.37 (2×1/6H, d, J=16 Hz), 4.32 (2×1/3H, d, J=15Hz), 4.62 (2×1/3H, d, J=15 Hz), 5.12-5.22 (1H, m), 6.78-7.27 (9H, m),8.08 (1×1/3H, d, J=8 Hz), 8.17 (1×2/3H, d, J=8 Hz)

(6) NMR (CDCl₃, δ): 2.19 (3×1/3H, s), 2.21 (3×2/3H, s), 2.28 (3H, s),2.31-2.47 (5H, m), 2.62-2.85 (1H, m), 2.72 (3×2/3H, s), 2.92 (3×1/3H,s), 2.95-3.18 (2H, m), 3.33-3.72 (5H, m), 4.30 (2×1/3H, s), 4.48(2×1/3H, d, J=15 Hz), 4.59 (2×1/3H, d, J=15 Hz), 5.02 (1×1/3H, q, J=8Hz), 5.12 (1×2/3H, q, J=8 Hz), 6.78-6.80 (1H, m), 7.07-7.17 (4H, m),7.20-7.30 (4H, m), 7.97 (1×1/3H, d, J=8 Hz), 8.13 (1×2/3H, d, J=8 Hz)

(7) MASS: 455 (M+1); NMR (CDCl₃, δ): 2.39-2.61 (1H, m), 2.70-2.82 (1H,m), 2.88 (3×3/4H, s), 2.89 (3×1/4H, s), 2.93-3.22 (2H, m), 3.38-3.47(2H, m), 3.51-3.73 (7H, m), 4.32 (2×1/6H, d, J=17 Hz), 4.48 (2×1/3H, d,J=15 Hz), 4.62 (2×1/6H, d, J=17 Hz), 4.64 (2×1/3H, d, J=15 Hz),4.93-5.04 (1×1/4H, m), 5.17-5.22 (1×3/4H, m), 6.82 (1×1/4H, d, J=5 Hz),6.88 (1×3/4H, d, J=5Hz), 7.17-7.31 (5H, m), 8.08-8.14 (1H, m), 8.58(1×1/4H, d, J=5 Hz), 8.60 (1×3/4H, d, J=5 Hz), 9.10 (1H, s)

(8) MASS: 505 (M+1); NMR (CDCl₃, δ): 2.28-2.36 (1×1/4H, m), 2.48-2.57(1×3/4H, m), 2.64-2.82 (1H, m), 2.86 (3×3/4H, s), 2.97 (3×1/4H, s),3.00-3.26 (2H, m), 3.35-3.48 (2H, m), 3.50-3.77 (7H, m), 4.68 (2×1/6H,d, J=16 Hz), 4.70 (2×1/3H, d, J=15 Hz), 4.81 (2×1/6H, d, J=16 Hz), 4.92(2×1/3H, d, J=15 Hz), 5.13-5.30 (1H, m), 7.09-7.22 (5H, m), 7.72-7.80(2H, m), 7.97-8.03 (1H, m), 8.08-8.20 (2H, m), 8.69 (1×1/4H, s), 8.78(1×3/4H, s)

(9) MASS: 504 (M+1); NMR (CDCl₃, δ): 2.23-2.33 (1×1/3H, m), 2.47-2.53(1×2/3H, m), 2.69-2.83 (1H, m), 2.85 (3×3/4H, s), 2.95 (3×1/4H, s),3.00-3.27 (2H, m), 3.37-3.47 (2H, m), 3.50-3.77 (7H, m), 4.65 (2×1/6H,d, J=16 Hz), 4.70 (2×1/3H, d, J=15 Hz), 4.72 (2×1/6H, d, J=16 Hz), 4.91(2×1/3H, d, J=15 Hz), 5.20-5.30 (1H, m), 7.11-7.23 (6H, m), 7.52 (1H, t,J=8 Hz), 7.70 (1H, t, J=8 Hz), 7.80 (1H, d, J=8 Hz), 8.00-8.20 (3H, m)

(10) MASS: 504 (M+1);. NMR (CDCl₃, δ): 2.29-2.52 (1H, m), 2.69-2.83 (1H,m), 2.80 (3×3/4H, s), 2.91 (3×1/4H, s), 2.98-3.18 (2H, m), 3.35-3.47(2H, m), 3.50-3.68 (7H, m), 4.42 (2×1/6H, d, J=16 Hz), 4.61 (2×1/6H, d,J=16 Hz), 4.68 (2×1/3H, d, J=15 Hz), 4.77 (2×1/3H, d, J=15 Hz),5.14-5.28 (1H, m), 7.11-7.30 (6H, m), 7.40 (1H, dd, J=8, 5 Hz), 7.72(1H, dd, J=8, 2 Hz), 7.78 (1×1/4H, s), 7.82 (1×3/4H, s), 8.08-8.20 (2H,m), 8.88-8.92 (1H, m)

(11) MASS: 455 (M+1); NMR (CDCl₃, δ): 2.31-2.40 (1×1/4H, m), 2.48-2.56(1×3/4H, m), 2.69-2.82 (1H, m), 2.85 (3×4/5H, s), 2.91 (3×1/5H, s),2.97-3.20 (2H, m), 3.36-3.42 (2H, m), 3.50-3.72 (7H, m), 4.43 (2×1/6H,d, J=16 Hz), 4.51 (2×1/3H, d, J=15 Hz), 4.62 (2×1/6H, d, J=16 Hz), 4.73(2×1/3H, d, J=15 Hz), 5.12-5.22 (1H, m), 7.15-7.29 (5H, m), 8.08-8.16(1H, m), 8.33-8.50 (3H, m)

(12) MASS: 531 (M+1); NMR (CDCl₃, δ): 2.47-2.60 (1H, m), 2.72 (3×3/4H,s), 2.81 (1H, dd, J=15, 2 Hz) 2.85 (3×1/4H, s), 2.97-3.11 (2H, m),3.40-3.48 (2H, m), 3.51-3.77 (7H, m), 4.32 (2×1/6H, d, J=16 Hz), 4.41(2×1/6H, d, J=16 Hz), 4.42 (2×1/3H, d, J=15 Hz), 4.65 (2×1/3H, d, J=15Hz), 5.11-5.22 (1H, m), 7.18-7.30 (5H, m), 7.38-7.42 (1H, m), 7.49 (1H,d, J=8 Hz), 7.61 (1×1/4H, d, J=8 Hz), 7.67 (1×3/4H, d, J=8 Hz), 8.18(1H, d, J=8 Hz), 8.27-8.32 (1H, m), 8.40 (1×1/4H, s), 8.50 (1×3/4H, s),8.67 (1H, d, J=5 Hz), 9.16 (1×1/4H, s), 9.18 (1×3/4H, s)

(13) MASS: 531 (M+1); NMR (CDCl₃, δ): 2.42-2.58 (1H, m), 2.67 (3×5/6H,s), 2.72-2.82 (1H, m), 2.83 (3×1/6H, s), 2.99-3.20 (2H, m), 3.41-3.48(2H, m), 3.52-3.77 (7H, m), 4.36 (2×1/6H, d, J=17 Hz), 4.38 (2×1/3H, d,J=15 Hz), 4.42 (2×1/6H, d, J=17 Hz), 4.71 (2×1/3H, d, J=15 Hz),5.12-5.23 (1H, m), 7.15-7.32 (6H, m), 7.51 (1H, d, J=8 Hz), 7.79-7.85(1H, m), 8.18 (1H, t, J=8 Hz), 8.27-8.40 (2H, m), 8.49 (1H, s), 8.70(1H, d, J=5 Hz)

(14) NMR (CDCl₃, δ): 0.89-1.00 (6H, m), 2.10 (1H, m), 2.72 (1H, dd, J=7,15 Hz), 2.84 (1H, dd, J=3, 15 Hz), 2.93 (3H×1/3, s), 3.04 (3H×2/3, s),3.47 (2H, m), 3.58-3.76 (7H, m), 4.38 (1H×2/3, d, J=15 Hz), 4.66(2H×1/3, s), 4.79 (1H, t, J=7 Hz), 4.83 (1H×2/3, d, J=15 Hz), 7.22-7.37(5H m), 8.12 (1H, m)

(15) NMR (CDCl₃, δ): 0.84-1.23 (3H, m), 1.51-1.94 (10H, m), 2.56-2.67(1H, m), 2.82-2.90 (1H, m), 2.94 (3H×1/3, s), 3.02 (3H×2/3, s), 3.46(2H, m), 3.62-3.76 (7H, m), 4.41 (1H×2/3, d, J=15 Hz), 4.58 (1H×1/3, d,J=16 Hz), 4.73 (1H×1/3, d, J=16 Hz), 4.77 (1H×2/3, d, J=15 Hz), 5.01(1H, m), 7.20-7.38 (5H, m), 7.91 (1H×1/3, d, J=7 Hz), 7.97 (1H×2/3, d,J=7 Hz)

(16) NMR (CDCl₃, δ): 2.34 (3H, s), 2.47 (1H, dd, J=7, 15 Hz), 2.57 (4H,m), 2.64 (3H×2/3, s), 2.76 (1H, dd, J=4, 7 Hz), 2.83 (3H×1/3, s),2.93-3.12 (2H, m), 3.19 (4H, m), 3.42 (2H, m), 3.66 (7H, m), 4.17(1H×1/3, d, J=16 Hz), 4.27 (1H×2/3, d, J=15 Hz), 4.33 (1H×1/3, d, J=16Hz), 4.55 (1H×2/3, d, J=15 Hz), 5.10-5.25 (1H, m), 6.81-7.03 (4H, m),7.15-7.25 (5H, m), 8.07 (1H×1/3, d, J=7 Hz), 8.13 (1H×2/3, d, J=7 Hz)

(17) NMR (CDCl₃, δ): 2.34-2.77 (2H, m), 2.79 (3H×2/3, s), 2.93 (3H×1/3,s), 2.87-3.14 (2H, m), 3.34-3.42 (2H, m), 3.50-3.68 (6H, m), 4.29(1H×2/3, d, J=15 Hz), 4.42 (1H×1/3, d, J=16 Hz), 4.57 (1H×1/3, d, J=16Hz), 4.72 (1H×2/3, d, J=15 Hz), 5.18 (1H, m), 6.97-7.15 (4H, m),7.26-7.31 (3H, m), 8.08 (1H×1/3, d, J=8 Hz), 8.20 (1H×2/3, d, J=8 Hz),8.43 (2H, d, J=5 Hz)

(18) NMR (CDCl₃, δ): 2.42-2.57 (1H, m), 2.72 (3H×3/4, s), 2.77-2.83 (1H,m), 2.85 (3H×1/4, s), 2.95-3.18 (2H, m), 3.43 (2H, m), 3.63 (6H, m),3.72 (1H, m), 4.38 (2H×1/4, s), 4.40 (1H×3/4, s), 4.67 (1H×3/4, s), 5.17(1H, m), 7.05-7.25 (7H, m), 7.57 (2H, m), 8.10 (1H, s), 8.17 (1H, t, J=8Hz), 8.54 (1H, s)

(19) MASS (m/z): 504 (M+H)⁺ ; NMR (CDCl₃, δ): 2.38-2.62 (1H, m),2.69-2.86 (1H, m), 2.72 (3/4×3H, s), 2.90 (1/4×3H, s), 2.94-3.22 (2H,m), 3.35-3.78 (9H, m), 4.53 (1/4×2H, ABq, Δ=0.10, J=17 Hz), 4.54(3/4×1H, d, J=15 Hz), 4.80 (3/4×1H, d, J=15 Hz), 5.10-5.29 (1H, m),7.06-7.30 (5H, m), 7.50-8.22 (6H, m), 8.64 (1/4×1H, d, J=2 Hz), 8.76(3/4×1H, d, J=2 Hz)

(20) MASS (m/z): 504 (M+H)⁺ ; NMR (CDCl₃, δ): 2.36-2.61 (1H, m),2.70-2.86 (1H, m), 2.72 (2/3×3H, s), 2.91 (1/3×3H, s), 2.92-3.20 (2H,m), 3.33-3.80 (9H, m), 4.51 (2/3×1H, d, J=15 Hz), 4.54 (1/3×2H, s), 4.85(2/3×1H, d, J=15 Hz), 5.13-5.28 (1H, m), 7.10-7.60 (8H, m), 7.98-8.25(3H, m), 8.90 (1H, d, J=2 Hz)

(21) MASS (m/z): 511. (M+H)⁺ ; NMR (CDCl₃, δ): 2.21 (3H, s), 2.40-2.61(1H, m), 2.66 (3/4×3H, s), 2.70-2.86 (1H, m), 2.78 (1/4×3H, s),2.92-3.20 (2H, m), 3.34-3.78 (9H, m), 4.24 (1/4×2H, ABq, Δ=0.16, J=17Hz), 4.28 (3/4×1H, d, J=15 Hz), 4.59 (3/4×1H, d, J=15 Hz), 5.05-5.22(1H, m), 7.10-7.45 (6H, m), 7.91-8.24 (4H, m)

(22) NMR (CDCl₃, δ): 1.80-2.00 (2H, m), 2.22-2.32 (1H, m), 2.30 (3H, s),2.33-2.42 (4H, m), 2.63 (3×2/3H, s), 2.90 (3×1/3H, s), 2.92-3.12 (2H,m), 3.27-3.40 (1H, m), 3.36-3.47 (2H, m), 3.53-3.70 (2H, m), 4.32-4.43(3×2/3H, m), 4.70 (3×1/3H, d, J=15 Hz), 5.19 (1H, q, J=8 Hz), 7.01-7.12(2H, m), 7.20-7.32 (8H, m), 7.93 (1×1/3H, d, J=8 Hz), 8.00 (1×2/3H, d,J=8 Hz)

(23) NMR (CDCl₃, δ): 2.53-3.03 (4H, m), 3.46 (2H, m), 3.66 (6H, m),3.79-3.89 (1H, m), 4.61-4.71 (1H, m), 4.93 (1H, d, J=16 Hz), 5.42 (1H,d, J=16 Hz), 6.92 (1H, d, J=8 Hz), 7.01 (1H, t, J=8 Hz), 7.14 (IH, t,J=8 Hz), 7.20-7.32 (6H, m), 8.45 (1H, t, J=7 Hz)

(24) MASS (m/z): 459 (M+1)⁺ ; NMR (CDCl₃, δ): 2.40-2.63 (1H, m),2.73-2.94 (1H, m), 2.84 (3H×2/3, s), 2.92 (3H×1/3, s), 3.11-3.50 (5H,m), 3.51-3.79 (7H, m), 4.39 (1H×2/3, d, J=14.5 Hz), 4.50 (1H×2/3, s),4.70 (1H×2/3, d, J=14.5 Hz), 5.10-5.23 (1H, m), 6.79-6.96 (2H, m),7.01-7.20 (3H, m), 7.22-7.35 (4H, m), 8.12 (1H×1/3, br d, J=7.5 Hz),8.21 (1H×2/3, br d, J=7.5 Hz)

(25) MASS (m/z): 533 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28-2.55 (1H, m), 2.67(2/3×3H, s), 2.69-2.85 (1H, m), 2.87 (1/3×3H, s), 2.92-3.16 (2H, m),3.33-3.79 (9H, m), 3.94 (3H, s), 4.32 (2/3×1H, d, J=15 Hz), 4.36(1/3×2H, ABq, Δ=0.08, J=17 Hz), 4.71 (2/3×1H, d, J=15 Hz), 5.10-5.25(1H, m), 6.50 (1/3×1H, d, J=2 Hz), 6.52 (2/3×1H, d, J=2 Hz), 6.95-7.42(8H, m), 7.65-7.75 (2H, m), 8.02-8.21 (1H, m)

(26) MASS (m/z): 497 (M+H)⁺ ; NMR (CDCl₃, δ): 2.33-2.52 (1H, m), 2.61(2/3×3H, s), 2.71-2.86 (1H, m), 2.76 (1/3×3H, s), 2.91-3.15 (2H, m),3.05 (1/3×6H, s), 3.07 (2/3×6H, s), 3.35-3.76 (9H, m), 3.95 (1/3×1H, d,J=17 Hz), 4.28 (1/3×1H, d, J=17 Hz), 4.34 (2/3×2H, ABq, Δ=0.22, J=15Hz), 5.03-5.33 (1H, m), 6.41 (1/3×1H, d, J=9 Hz), 6.46 (2/3×1H, d, J=9Hz), 7.02-7.33 (6H, m), 7.88 (1/3×1H, d, J=2 Hz), 7.97 (2/3×1H, d, J=2Hz), 8.06-8.19 (1H, m)

(27) MASS (m/z): 519 (M+H)⁺ ; NMR (CDCl₃, δ): 2.40-2.62 (1H, m),2.70-2.85 (1H, m), 2.72 (3/4×3H, s), 2.85 (1/4×3H, s), 2.92-3.22 (2H,m), 3.35-3.79 (9H, m), 4.37 (1/4×2H, s), 4.53 (3/4×2H, ABq, Δ=0.22, J=15Hz), 5.08-5.25 (1H, m), 6.98-7.33 (1H, m), 7.82 (1H, s), 8.10-8.22 (1H,m)

(28) MASS (m/z): 521 (M+H)⁺ ; NMR (CDCl₃, δ): 2.26-2.52 (1H, m), 2.59(3H, s), 2.66 (3/5×3H, s), 2.68-2.82 (1H, m), 2.83 (2/5×3H, s),2.92-3.16 (2H, m), 3.35-3.80 (9H, m), 3.70 (2/5×3H, s), 3.72 (3/5×3H,s), 4.23 (2/5×1H, d, J=17 Hz), 4.56 (2/5×1H, d, J=17 Hz), 4.61 (3/5×2H,ABq, Δ=0.07, J=15 Hz), 5.06-5.25 (1H, m), 6.86-7.50 (8H, m), 8.05-8.22(1H, m)

(29) MASS (m/z): 443 (M+H)⁺ ; NMR (CDCl₃, δ): 2.43-2.67 (1H, m),2.71-3.03 (3H, m), 2.90 (2/3×3H, s), 2.92 (1/3×3H, s), 3.33-3.78 (9H,m), 4.38 (2/3×1H, d, J=15 Hz), 4.54 (1/3×2H, ABq, Δ=0.08, J=17 Hz), 4.72(2/3×1H, d, J=15 Hz), 5.02-5.16 (1H, m), 6.22 (1/3×1H, s), 6.29 (2/3×1H,s), 7.03-7.39 (7H, m), 8.02-8.23 (1H, m)

(30) MASS (m/z): 457 (M+H)⁺ ; NMR (CDCl₃, δ): 2.38-2.57 (1H, m), 2.69(2/3×3H, s), 2.71-2.87 (1H, m), 2.84 (1/3×3H, s), 2.90-3.20 (2H, m),3.36-3.75 (9H, m), 3.80 (1/3×3H, s), 3.87 (2/3×3H, s), 4.15 (2/3×1H, d,J=15 Hz), 4.15 (1/3×2H, ABq, Δ=0.07, J=17 Hz), 4.45 (2/3×1H, d, J=15Hz), 5.02-5.29 (1H, m), 6.98-7.35 (7H, m), 8.04-8.20 (1H, m)

(31) MASS (m/z): 487 (M+H)⁺ ; NMR (CDCl₃, δ): 2.25-2.58 (1H, m),2.58-2.80 (1H, m), 2.77 (2/3×3H, s), 2.82-3.14 (2H, m), 2.91 (1/3×3H,s), 3.30-3.80 (9H, m), 4.30 (2/3×1H, d, J=15 Hz), 4.49 (1/3×2H, ABq,Δ=0.15, J=17 Hz), 4.72 (2/3×1H, d, J=15 Hz), 5.05-5.23 (1H, m),6.90-7.40 (9H, m), 8.04 (1/3×1H, d, J=9 Hz), 8.15 (2/3×1H, d, J=9 Hz)

(32) MASS (m/z): 443 (M+H)⁺ ; NMR (CDCl₃, δ): 2.41-2.64 (1H, m),2.73-2.96 (1H, m), 2.83 (2/3×3H, s), 2.90 (1/3×3H, s), 2.96-3.20 (2H,m), 3.38-3.81 (9H, m), 4.33 (2/3×1H, d, J=15 Hz), 4.50 (1/3×2H, ABq,Δ=0.07, J=17 Hz), 4.79 (2/3×1H, d, J=15 Hz), 5.15-5.31 (1H, m), 6.10(1H, m), 6.21-6.31 (1H, m), 7.07-7.40 (6H, m), 8.11 (1/3×1H, d, J=8 Hz),8.19 (2/3×1H, d, J=8 Hz)

(33) MASS: 505 (M+1); NMR (CDCl₃, δ): 2.38-2.60 (1H, m), 2.78 (3×2/3H,s), 2.79 (1H, t, J=16 Hz), 2.91 (3×1/3H, s), 2.98-3.19 (2H, m),3.38-3.49 (2H, m), 3.52-3.70 (6H, m), 3.71-3.80 (1H, m), 4.51 (2×1/6H,d, J=16 Hz), 4.60 (2×1/6H, d, J=16 Hz), 4.65 (2×1/3H, d, J=15 Hz), 4.81(2×1/3H, d, J=15 Hz), 5.13-5.28 (1H, m), 7.13-7.29 (5H, m), 7.31(1×1/3H, d, J=8 Hz), 7.43 (1×2/3H, d, J=8 Hz), 7.78 (1×1/3H, s), 7.83(1×2/3H, s), 7.99-8.03 (1H, m), 8.14 (1×1/3H, d, J=8 Hz), 8.19 (1×2/3H,d, J=8 Hz), 8.82 (2H, s)

(34) MASS: 503 (M+1); NMR (CDCl₃, δ): 2.12 (3×2/3H, s), 2.19-2.30(1×1/3H, s), 2.41-2.51 (1×2/3H, s), 2.68-2.89 (1H, m), 2.79 (3×1/3H, s),3.30-3.48 (3H, m), 3.52-3.79 (8H, m), 4.03 (2×1/6H, d, J=16 Hz), 4.27(2×1/6H, d, J=16 Hz), 4.28 (2×1/3H, d, J=15 Hz), 4.49 (2×1/3H, d, J=15Hz), 5.29-5.41 (1H, m), 6.77-6.83 (2×1/3H, m), 6.93-7.02 (2×2/3H, m),7.13-7.31 (5H, m), 7.32-7.60 (3H, m), 7.69-7.87 (2H, m), 8.30-8.39 (1H,m)

(35) MASS: 454 (M+1); NMR (CDCl₃, δ): 2.33-2.60 (1H, m), 2.62-2.79 (1H,m), 2.80 (3×2/3H, s), 2.92 (3×1/3H, s), 2.88-3.19 (2H, m), 3.33-3.48(2H, m), 3.49-3.72 (7H, m), 4.40 (2×1/3H, d, J=15 Hz), 4.45 (2×1/6H, d,J=16 Hz), 4.53 (2×1/6H, d, J=16 Hz), 4.63 (2×1/3H, d, J=15 Hz),5.08-5.22 (1H, m), 6.98-7.20 (3H, m), 7.22-7.37 (3H, m), 7.43 (1×1/3H,d, J=8 Hz), 7.51 (1×2/3H, d, J=8 Hz), 8.11 (1×1/3H, d, J=8 Hz), 8.22(1×2/3H, d, J=8 Hz), 8.36 (1×1/3H, s), 8.45 (1×2/3H, s), 8.45 (1H, s)

(36) MASS: 484 (M+1); NMR (CDCl₃, δ): 2.43-2.70 (1H, m), 2.61 (3×3/4H,s), 2.73-2.88 (1H, m), 2.79 (3×1/4H, s), 2.93-3.18 (2H, m), 3.40-3.49(2H, m), 3.51-3.70 (6H, m), 3.71-3.80 (1H, m), 3.91 (3H, s), 4.10(2×1/6H, d, J=16 Hz), 4.23 (2×1/3H, d, J=15 Hz), 4.30 (2×1/6H, d, J=16Hz), 4.53 (2×1/3H, d, J=15 Hz), 5.03-5.23 (1H, m), 6.59-6.70 (1H, m),7.07-7.33 (6H, m), 7.83 (1×1/4H, s), 7.93 (1×3/4H, s), 8.10-8.22 (1H, m)

(37) MASS: 419 (M+1); NMR (CDCl₃, δ): 0.79-1.00 (3H, m), 1.15-1.48 (4H,m), 1.55-1.90 (2H, m), 2.58-2.72 (1H, m), 2.80-2.90 (1H, m), 2.92(3×1/3H, s), 2.97 (3×2/3H, s), 3.40-3.50 (2H, m), 3.51-3.70 (6H, m),3.71-3.79 (1H, m), 4.43 (2×1/3H, d, J=15 Hz), 4.60 (2×1/6H, d, J=16 Hz),4.68 (2×1/6H, d, J=16 Hz), 4.75 (2×1/3H, d, J=15 Hz), 4.86-4.99 (1H, m),7.17-7.40 (5H, m), 8.07 (1×1/3H, d, J=8 Hz), 8.12 (1×2/3H, d, J=8 Hz)

Preparation 67

Starting Compound (1.14 g) was dissolved in 30% methylamine in methanol(7 ml) and heated at 50° C. for 1 hour. After the mixture was allowed tocool to room temperature, the solvent was evaporated then suspended inethanol (15 ml). Sodium borohydride (277 mg) was added to the suspensionwith ice-cooling, and the mixture was stirred at 0° C. for 1 hour. Afterthe solvent was evaporated, the residue was diluted with water,extracted three times with chloroform, and dried over magnesium sulfate.Evaporation of the solvent followed by column chromatography (silicagel, chloroform/methanol=5/1) gave Object Compound (708 mg) as acolorless oil.

MASS (m/z): 173 (M+H)⁺ ; NMR (CDCl₃, δ): 2.51 (3H, s), 3.96 (2H, s),7.48-7.85 (3H, m), 8.05-8.14 (2H, m), 8.89 (1H, d, J=2 Hz)

Preparation 68

Starting Compound (1.30 g) was dissolved in 30% methylamine in methanol(8 ml) and heated at 60° C. for 1 hour. After the mixture was allowed tocool to room temperature, the solvent was evaporated then suspended inethanol (20 ml). The suspension was cooled in ice and added sodiumborohydride (305 mg). The mixture was stirred at the temperature for 1hour and the solvent was evaporated. The residue was diluted with water,and extracted three times with chloroform. The organic layer was washedwith brine and dried over potassium carbonate. Evaporation of thesolvent followed by column chromatography (silica gel,chloroform/methanol=5/1) gave Object Compound (923 mg) as a light yellowoil.

MASS (m/z): 180 (M+H)⁺ ; NMR (CDCl₃, δ): 2.18 (3H, s), 2.43 (3H, s),3.70 (2H, s), 7.67 (1H, dd, J=9, 2 Hz), 8.15 (1H, d, J=9 Hz), 8.20 (1H,d, J=2 Hz), 8.31 (1H, br s)

Preparation 69

The following object compounds were obtained according to a similarmanner to that of Preparation 22, 23, 25, 67 or 68.

(1) MASS (m/z): 2 20 (M⁺ +1); NMR (CDCl₃, δ): 2.35 (3H, s), 2.44 (3H,s), 2.57 (4H, t, J=5 Hz), 3.19 (4H, t, J=5 Hz), 3.65 (2H, s), 6.89 (2H,d, J=8 Hz), 7.21 (2H, d, J=8 Hz)

(2) MASS (m/z): 173 (M+H)⁺ ; NMR (CDCl₃, δ): 2.51 (3H, s), 3.96 (2H, s),7.40 (1H, dd, J=9, 5 Hz), 7.70 (1H, d, J=9 Hz), 7.77 (1H, s), 8.08 (1H,d, J=9 Hz), 8.13 (1H, d, J=9 Hz), 8.89 (1H, d, J=5 Hz)

(3) Mass: 200 (M+1); NMR (CDCl₃, δ): 2.45 (3H, s), 3.81 (2H, s),7.28-7.32 (1H, m), 7.80 (2H, t, J=7 Hz), 8.36 (1H, d, J=7 Hz), 8.38 (1H,d, J=7 Hz), 8.61 (1H, s), 8.67 (1H, d, J=5 Hz)

(4) MASS: 200 (M+1); NMR (CDCl₃, δ): 2.49 (3H, s), 3.80 (2H, s), 7.39(1H, dd, J=8, 5 Hz), 7.63 (1H, d, J=8 Hz), 7.80 (1H, dd, J=8, 2 Hz),8.31 (1H, dd, J=8, 2 Hz), 8.63-8.68 (2H, m), 9.20 (1H, s)

(5) MASS: 125 (M+2); NMR (CDCl₃, δ): 2.50 (3H, s), 3.90 (2H, s), 8.51(2H, d, J=16 Hz), 8.62 (1H, s)

(6) MASS: 173 (M+1); NMR (CDCl₃, δ): 2.52 (3H, s), 4.00 (2H, s), 7.38(1H, dd, J=8, 3 Hz), 7.58 (1H, d, J=8 Hz), 7.80 (1H, d, J=8 Hz), 7.99(1H, s), 8.13 (1H, d, J=8 Hz), 8.90 (1H, d, J=5 Hz)

(7) MASS: 173 (M+1); NMR (CDCl₃, δ): 2.52 (3H, s), 4.07 (2H, s), 7.46(1H, d, J=8 Hz), 7.51 (1H, t, J=8 Hz), 7.70 (1H, t, J=8 Hz), 7.80 (1H,d, J=8 Hz), 8.07 (1H, d, J=8 Hz), 8.12 (1H, d, J=8 Hz)

(8) MASS: 174 (M+1); NMR (CDCl₃, δ): 2.58 (3H, s), 4.12 (2H, s),7.70-7.80 (2H, m), 8.03-8.12 (2H, m), 8.90 (1H, s)

(9) MASS: 125 (M+1); NMR (CDCl₃, δ): 2.49 (3H, s), 3.89 (2H, s), 7.37(1H, d, J=7 Hz), 8.67 (1H, d, J=7 Hz), 9.17 (1H, s)

(10) MASS: 173 (M+1); NMR (CDCl₃, δ): 2.48 (3H, s), 4.00 (2H, s), 7.80(1H, d, J=8 Hz), 8.02 (1H, s), 8.09 (1H, d, J=8 Hz), 8.80-8.87 (2H, m)

(11) MASS (m/z): 126 (M+H)⁺ ; NMR (CDCl₃, δ): 2.45 (3H, s), 3.61 (2H,s), 3.87 (3H, s), 7.29 (1H, s), 7.41 (1H, s)

(12) mp: 102-103° C.; MASS (m/z): 159 (M-30)⁺, 190 (M+H)⁺ ; NMR (CDCl₃,δ): 2.45 (3H, s), 2.58 (3H, s), 3.70 (3H, s), 3.85 (2H, s), 7.22 (2H,s), 7.58 (1H, s)

(13) MASS (m/z): 188 (M+H)⁺ ; NMR (CDCl₃, δ): 2.48 (3H, s), 3.79 (2H,s), 7.19 (1H, s), 7.27 (1H, s), 7.35 (2H, d, J=8 Hz), 7.42 (2H, d, J=8Hz), 7.83 (1H, s)

(14) MASS (m/z): 166 (M+H)⁺ ; NMR (CDCl₃, δ): 2.42 (3H, s), 3.07 (6H,s), 3.61 (2H, s), 6.51 (1H, d, J=9 Hz), 7.46 (1H, dd, J=9, 2 Hz), 8.07(1H, d, J=2 Hz)

(15) MASS (m/z): 202 (M+H)⁺ ; NMR (CDCl₃, δ): 2.45 (3H, s), 3.78 (2H,s), 3.93 (3H, s), 6.52 (1H, d, J=2 Hz), 7.34 (2H, d, J=8 Hz), 7.37 (1H,d, J=2 Hz), 7.74 (2H, d, J=8 Hz)

Preparation 70

A slurry of Starting Compound (6.45 g), selenium dioxide (7.48 g), andwater (1.2 ml) in 285 ml of dioxane was refluxed for 6 days. The mixturewas filtered while still warm, and the filtrate was evaporated. Theresidue was purified using silica gel column chromatography (eluent:hexane/ethyl acetate (2:1)) yielding Object Compound (380 mg).

MASS: 158 (M+1); NMR (CDCl₃, δ): 7.52-7.67 (1H, m), 7.93 (1H, d, J=8Hz), 8.07 (1H, d, J=8 Hz), 8.23 (1H, d, J=8 Hz), 8.53 (1H, s), 9.03 (1H,d, J=5 Hz), 10.25 (1H, s)

Preparation 71

The following object compounds were obtained according to a similarmanner to that of Preparation 70.

(1) mp: 65-68° C.; NMR (CDCl₃, δ): 7.68 (1H, t, J=8 Hz), 7.82 (1H, t,J=8 Hz), 7.90 (1H, d, J=8 Hz), 8.02 (1H, d, J=8 Hz), 8.27 (1H, d, J=8Hz), 8.31 (1H, d, J=8 Hz), 10.22 (1H, s)

(2) mp: 108-109° C.; MASS: 159 (M+1); NMR (CDCl₃, δ): 7.87-7.99 (2H, m),8.18-8.29 (2H, m), 9.40 (1H, s), 10.29 (1H, s)

(3) NMR (CDCl₃, δ): 7.85 (1H, d, J=8 Hz), 9.04 (1H, d, J=8 Hz), 9.47(1H, s)

(4) mp: 137-139° C.; MASS: 159 (M+1); NMR (CDCl₃, δ): 8.23 (1H, d, J=8Hz), 8.29 (1H, d, J=8 Hz), 8.60 (1H, s), 8.97 (2H, s), 10.27 (1H, s)

Preparation 72

To a solution of-dimethylsulfoxide (0.86 ml) in dichloromethane (20 ml)was added oxalyl chloride (0.53 ml) at -78° C. After the solution wasstirred at -78° C. for 10 minutes, Starting Compound (900 mg) indichloromethane (10 ml) was added thereto. The solution was stirred at-78° C. for 15 minutes, and triethyl amine (3.7 ml) was added thereto.The solution was allowed to ambient temperature and stirred for 1 hour.Water was added thereto and the aqueous layer was extracted withchloroform. The organic layer was dried over magnesium sulfate andconcentrated. The residue was purified by chromatography on silica gelchloroform-methanol (30:1)! to give Object Compound (720 mg) as a solid.

mp: 85-88° C.; MASS: 185 (M+1); NMR (CDCl₃, δ): 7.37-7.42 (1H, m),7.82-7.90 (1H, m), 8.29 (1H, d, J=8 Hz), 8.51 (1H, d, J=8 Hz), 8.62 (1H,d, J=8 Hz), 8.72 (1H, d, J=5 Hz), 9.11 (1H, s), 10.11 (1H, s)

Preparation 73

The following object compounds were obtained according to a similarmanner to that of Preparation 72.

(1) NMR (CDCl₃, δ): 8.70 (2H, dd, J=12, 3 Hz), 9.19 (1H, s), 10.21 (1H,s)

(2) mp: 66-72° C.; MASS: 185 (M+1); NMR (CDCl₃, δ): 7.48 (1H, dd, J=8, 5Hz), 7.95 (1H, d, J=8 Hz), 8.29 (1H, dd, J=8, 5 Hz), 8.42 (1H, dd, J=8,2 Hz), 8.72 (1H, d, J=5 Hz), 9.17 (1H, d, J=2 Hz), 9.30 (1H, d, J=2 Hz),10.20 (1H, s)

Preparation 74

To a solution of Starting Compound (1.15 g) in anhydrous tetrahydrofuran(20 ml) at -78° C. was added 5.04 ml of a 1M solution of lithiumaluminium hydride in tetrahydrofuran. The reaction mixture was allowedto warm to the temperature (-20° C.) which the solution becamecompletely homogeneous. The reaction mixture was stirred at thistemperature for 30 minutes and then cooled back down to -78° C. andquenched slowly with 15 ml of 10% aqueous tetrahydrofuran. After beingwarmed to ambient temperature, the reaction mixture was stirred with dryCelite for 15 minutes and then filtered. The solution was thenconcentrated under reduced pressure. The residue was purified bychromatography on silica gel chloroform-methanol (10:1)! to give ObjectCompound (900 mg) as an oil.

MASS: 187 (M+1); NMR (CDCl₃, δ): 3.07 (1H, br s), 4.74 (2H, s),7.29-7.32 (1H, m), 7.78-7.85 (2H, m), 8.31 (2H, t, J=8 Hz), 8.57 (1H,s), 8.66 (1H, d, J=6 Hz)

Preparation 75

The following object compounds were obtained according to a similarmanner to that of Preparation 74.

(1) mp: 92-95° C.; MASS: 187 (M+1); NMR (CDCl₃, δ): 2.57 (1H, br s),4.80 (2H, s), 7.40 (1H, dd, J=12, 5 Hz), 7.70 (1H, dd, J=8 Hz), 7.81(1H, dd, J=8, 2 Hz), 8.29 (1H, dd, J=8, 2 Hz), 8.60 (1H, d, J=5 Hz),8.67 (1H, s), 9.02 (1H, s)

(2) MASS: 112 (M+2); NMR (CDCl₃, δ): 3.32 (1H, t, J=7 Hz), 4.87 (2H, d,J=7 Hz), 8.50-8.52 (2H, m), 8.62 (1H, s)

Preparation 76

To a mixture of Starting Compound (434 mg) andN,O-dimethylhydroxylaminehydrochloride (246 mg) indichloromethane-N,N-dimethylformamide (1:1, 5 ml) was added1-ethyl-3-(3-dimethylaminopropyl) carbodiimidehydrochloride (534 mg) atroom temperature. The reaction mixture was stirred at room temperaturefor 12 hours. The solution was diluted with ethyl acetate, washed twicewith saturated sodium bicarbonate, once with brine, and dried overmagnesium sulfate. Purification by flash chromatography (silica gel,hexane/ethyl acetate 1/3) gave Object Compound (303 mg, 55.8%) as anoil.

MASS (m/z): 217 (M+H)⁺ ; NMR (CDCl₃, δ): 3.42 (3H, s), 3.56 (3H, s),7.46 (1H, dd, J=9, 5 Hz), 8.06 (2H, ABq, Δ=0.12, J=9 Hz), 8.21 (1H, s),8.22 (1H, dd, J=9, 2 Hz), 8.98 (1H, dd, J=5, 2 Hz)

Preparation 77

To an ice-cooled solution of Starting Compound (543 mg) in dry ether(6.3 ml) was added lithium aluminum hydride (96 mg) and stirred at 0° C.for 1 hour. After the reaction mixture was diluted with ether, 10%citric acid (0.3 ml) was added dropwise with vigorous stirring. Theprecipitate was filtered off, and the residue was purified by columnchromatography (silica gel, hexane/ethyl acetate=1/1) to give theproduct (268 mg) as white crystals.

mp: 70-71° C.; MASS (m/z): 158 (M+H)⁺ ; NMR (CDCl₃, δ): 7.52 (1H, dd,J=9, 3 Hz), 8.21 (2H, ABq, Δ=0.04, J=9 Hz), 8.33 (1H, d, J=9 Hz), 8.36(1H, s), 9.05 (1H, d, J=3 Hz), 10.21 (1H, s)

Preparation 78

A mixture of Starting Compound (3.0 g), 1-methylpiperazine (2.7 g) andpotassium carbonate (4.0 g) in N,N-dimethylformamide (5 ml) was stirredat 120° C. for 2 hours. After cooling potassium carbonate was removed byfiltration. Evaporation of N,N-dimethylformamide in vacuo gave a residuewhich was taken up in chloroform and water. The organic solution waswashed with water, and dried. Evaporation of solvent gave a residuewhich was chromatographed on silica gel. Elution withmethanol-chloroform (1:50) afforded Object Compound (2.63 g)

MASS (m/z): 205 (M⁺ +1); NMR (CDCl₃, δ): 2.36 (3H, s), 2.55 (4H, t, J=5Hz), 3.41 (4H, t, J=5 Hz), 6.92 (2H, d, J=8 Hz), 7.75 (2H, d, J=8 Hz),9.78 (1H, s)

Preparation 79

The following object compounds were obtained according to a similarmanner to that of Preparation 29.

(1) MASS: 236 (M+1); NMR (CDCl₃, δ): 1.48 (9H, s), 2.26 (3H, s), 2.79(3H, s), 4.43 (2H, s), 7.09-7.19 (4H, m)

(2) MASS: 336 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.33 (3H, s), 2.80(3H, br s), 4.38 (2H, s), 6.97-7.08 (3H, m), 7.22 (1H, dd, J=15, 8 Hz)

Preparation 80

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8 or 41.

(1) MASS: 136 (M+1); NMR (CDCl₃, δ): 2.37 (3H, s), 2.51 (3H, s), 2.71(2H, s), 7.13-7.18 (3H, m), 7.23-7.30 (1H, m)

(2) MASS: 136 (M+1); NMR (CDCl₃, δ): 2.35 (3H, s), 2.43 (3H, s), 3.70(2H, s), 7.06-7.27 (4H, m)

Preparation 81

The following object compound was obtained accordidng to a similarmanner to that of Preparation 6.

MASS: 351 (M+1); NMR (CDCl₃, δ): 1.42 (9H, s), 2.87 (1H, dd, J=17, 5Hz), 2.91 (3H, s), 2.97 (3H, s), 3.17 (1H, dd, J=16, 5 Hz), 4.58-4.63(1H, m), 5.13 (2×1/2H, d, J=12 Hz), 5.21 (2×1/2H, d, J=12 Hz), 5.88 (1H,d, J=8 Hz), 7.29-7.37 (5H, s)

Preparation 82

The following object compound was obtained according to a similar mannerto that of Preparation 10.

MASS: 261 (M+1); NMR (CDCl₃, δ): 1.38 (9H, s), 2.67-2.77 (1H, m), 3.00(3H, s), 3.05 (3H, s), 3.21 (1H, d, J=15 Hz), 4.51 (1H, t, J=8 Hz), 5.88(1H, br s)

Preparation 83

The following object compound was obtained according to a similar mannerto that of Preparation 10.

NMR (CDCl₃, δ): 1.42 (9H, s), 1.82-1.98 (1H, m), 2.00-2.18 (1H, m),2.38-2.60 (2H, m), 2.70 (3×2/3H, s), 2.83 (3×1/3H, s), 3.00-3.15 (2H,m), 4.28-5.20 (3H, m), 5.21-5.30 (1H, m), 5.50-5.60 (1H, m), 6.90-7.00(2H, m), 7.09-7.30 (8H, m), 8.18-8.30 (1H, m)

Preparation 84

The following object compound was obtained according to a similar mannerto that of Preparation 1.

NMR (CDCl₃, δ): 1.47 (9H, s), 1.90-2.00 (1H, m), 2.00-2.20 (1H, m), 2.31(3H, s), 2.32-2.53 (6H, m), 2.63 (3×2/3H, s), 2.82 (3×1/3H, s),2.98-3.10 (2H, m), 3.40-3.48 (2H, m), 3.60-3.70 (2H, m), 4.07-4.18 (1H,m), 4.20 (2×1/4H, d, J=16 Hz), 4.32 (2×1/4H, d, J=16 Hz), 4.35 (2×1/4H,d, J=15 Hz), 4.61 (2×1/4H, d, J=15 Hz), 5.11 (1H, q, J=8 Hz), 5.58-5.66(1H, m), 6.98 (2×1/3H, d, J=8 Hz), 7.08 (2×2/3H, d, J=8 Hz), 7.12-7.31(8H, m), 7.45-7.55 (1H, m)

Preparation 85

The following object compound was obtained according to similar mannersto those of Preparations 10 and 6.

MASS (m/z): 567 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45 (9H, s), 1.8-2.2 (2H, m),2.3-2.6 (2H, m), 2.63 (2/3×3H, s), 2.84 (1/3×3H, s), 3.0-3.1 (2H, m),3.4-3.5 (2H, m), 3.6-3.7 (6H, m), 4.1-4.2 (1H, m), 4.28 (1/3×2H, ABq,Δ=0.20, J=15 Hz), 4.50 (2/3×2H, ABq, Δ=0.22, J=15 Hz), 5.1-5.2 (1H, m),5.5-5.6 (1H, m), 7.0-7.6 (11H, m)

Preparation 86

To a stirred suspension of sodium hydride (0.31 g, 60%) inN,N-dimethylformamide (10 ml) was added a solution of Starting Compound(0.7 g) in dimethylformamide (2 ml) at 0° C. The mixture was stirred atroom temperature for 1 hour. To this mixture was added dropwisebenzylbromide (0.63 g) at 0° C. The mixture was stirred at roomtemperature for 1 hour. The reaction mixture was poured into water andextracted with ethyl acetate. The organic layer was washed with waterand dried. Evaporation of solvent gave a residue which waschromatographed on silica gel. Elution with a mixture ofmethanol-chloroform (1:100) provided Object Compound (0.56 g).

MASS (m/z): 253 (M⁺ +1); NMR (CDCl₃, δ): 2.94 (1H, t, J=15 Hz), 3.15(1H, dd, J=5, 15 Hz), 3.72 (1H, dd, J=5, 15 Hz), 4.97 (1H, d, J=16 Hz),5.40 (1H, d, J=16 Hz), 6.88 (1H, d, J=8 Hz), 6.99 (1H, t, J=8 Hz), 7.13(1H, t, J=8 Hz), 7.20-7.33 (6H, m)

Preparation 87

A mixture of Starting Compuond (4.85 g) and N,N-dimethylformamidedimethyl acetal (17 ml) in benzene (12.5 ml) was distilled. Thedistillation was continued by occasional addition of benzene until mostof the starting material was consumed. Then water was added thereto, themixture was extracted three times with ether, washed with brine, anddried over magnesium sulfate. The product was purified by columnchromatography (silica gel, chloroform/methanol=30/1) followed byrecrystallization from toluene to give Object Compound (4.48 g) ofyellow crystals.

mp: 99-100° C.; MASS (m/z): 248 (M+H)⁺ ; NMR (CDCl₃, δ): 1.40 (3H, t,J=7 Hz), 2.95 (3H, br s), 3.18 (3H, br s), 4.40 (2H, q, J=7 Hz), 6.22(1H, d, J=13 Hz), 7.83 (1H, d, J=13 Hz), 7.92 (2H, d, J=7 Hz), 8.05 (2H,d, J=7 Hz)

Preparation 88

Starting compound (2.47 g) was dissolved in acetic acid (10 ml) andmethylhydrazine (519 mg) was added dropwise at room temperature. Thereaction mixture was stirred at the temperature for 1 hour. The mixturewas neutralized with 15% sodium hydroxide with ice-cooling, extractedthree times with ethyl acetate, washed with brine, and dried overmagnesium sulfate. The crude product was the 57:43 isomeric mixture ofObject Compound A and Object Compound B determined by NMR. The twoisomers were separated by column chromatography (silica gel,chloroform), and the first eluate was Object Compound A as whitecrystals (1.11 g) and the second was Object Compound B as an oil (646mg).

Object Compound A

mp: 79-80° C.; MASS (m/z): 231 (M+H)⁺ ; NMR (CDCl₃, δ): 1.41 (3H, t, J=7Hz), 3.97 (3H, s), 4.38 (2H, q, J=7 Hz), 6.60 (1H, d, J=2 Hz), 7.40 (1H,d, J=2 Hz), 7.85 (2H, d, J=7 Hz), 8.06 (2H, d, J=7 Hz)

Object Compound B

MASS (m/z): 231(M+H)⁺ ; NMR (CDCl₃, δ): 1.41 (3H, t, J=7 Hz), 3.91 (3H,s), 4.41 (2H, q, J=7 Hz), 6.37 (1H, d, J=1 Hz), 7.49 (2H, d, J=7 Hz),7.52 (1H, d, J=1 Hz), 8.12 (2H, d, J=7 Hz)

Preparation 89

To an ice-cooled suspension of lithium aluminum hydride (183 mg) intetrahydrofuran (12 ml) was added Starting Compound (1.08 g) intetrahydrofuran (12 ml). After the mixture was stirred at 0° C. for 1hour, sodium fluoride (790 mg) and water (0.25 ml) were successivelyadded thereto and the whole was stirred at room temperature for 1 hour.The precipitate formed was filtered off, and the resulting solution wasevaporated to give Object Compound (876 mg) as white crystals.

mp: 92-93° C.; MASS (m/z): 189 (M+H)⁺ ; NMR (CDCl₃, δ): 3.92 (3H, s),4.69 (2H, d, J=5 Hz), 6.52 (1H, d, J=1 Hz), 7.36 (1H, d, J=1 Hz), 7.38(2H, d, J=8 Hz), 7.77 (2H, d, J=8 Hz)

Preparation 90

To an acetone (45 ml) solution of Starting Compound (846 mg) was addedactivated manganese dioxide powder (7.82 g) and the mixture was refluxedfor 1 hour. After the mixture was filtered, the Object Compound wasisolated by column chromatography (silica gel, hexane/ethyl acetate=1/1)as white crystals (550 mg).

mp: 88-90° C.; MASS (m/z): 187 (M+H)⁺ ; NMR (CDCl₃, δ): 3.97 (3H, s),6.62 (1H, d, J=2 Hz), 7.41 (1H, d, J=2 Hz), 7.82-8.03 (4H, m), 10.01(1H, s)

Preparation 91

To a methanol (20 ml) solution of Starting Compound (2.36 g) was added50% aqueous dimethylamine solution (20 ml), and the mixture was refluxedfor 12 hours. After the methanol was evaporated, sodium chloride wasadded thereto, and the mixture was extracted three times with ether. Theorganic layer was dried over magnesium sulfate. Evaporation of thesolvent followed by column chromatography (silica gel, hexane/ethylacetate=20/1) gave Object Compound (1.39 g) as white crystals.

mp: 40-41° C.; MASS (m/z): 201, 203 (M+H)⁺ ; NMR (CDCl₃, δ): 3.03 (6H,s), 6.39 (1H, d, J=9 Hz), 7.47 (1H, dd, J=9, 2 Hz), 8.14 (1H, d, J=2 Hz)

Preparation 92

To a stirred solution of Starting Compound (1.33 g) in tetrahydrofuran(16.5 ml) at -78° C. was added n-butyllithium (1.6M in hexane, 4.4 ml).After 2 hours, N,N-dimethylformamide (968 mg) was added thereto and thestirring was continued for 1 hour at -78° C. To the cold mixture wasadded saturated sodium- hydrogen carbonate solution (20 ml) and themixture was extracted three times with ether. The organic layer wasdried over magnesium sulfate. Evaporation of the solvent followed bycolumn chromatography (hexane/ethyl acetate=2/1) gave Object Compound(777 mg) as white crystals.

mp: 44-45° C.; MASS (m/z): 151 (M+H)⁺ ; NMR (CDCl₃, δ): 3.20 (6H, s),6.56 (1H, d, J=9 Hz), 7.91 (1H, dd, J=9, 2 Hz), 8.55 (1H, d, J=2 Hz),9.76 (1H, s)

Preparation 93

A mixture of 4-fluorobenzonitrile (6.05 g), imidazole (4.09 g), andpotassium carbonate (8.33 g) in N,N-dimethylformamide (50 ml) was heatedat 120° C. for 2 hours. The mixture was cooled and evaporated. Then themixture was diluted with water (50 ml), added 1N sodium hydroxidesolution to make basic, and extracted three times with ethyl acetate.The organic layer was dried over magnesium sulfate. Evaporation of thesolvent followed by column chromatography (silica gel, ethyl acetate)gave Object Compound (7.75 g) as white crystals.

mp: 151-152° C.; MASS (m/z): 170 (M+H)⁺ ; NMR (CDCl₃, δ): 7.26 (1H, s),7.32 (1H, s), 7.53 (2H, d, J=8 Hz), 7.80 (2H, d, J=8 Hz), 7.93 (1H, s)

Preparation 94

To a stirred solution of Starting Compound (4.23 g) in dichloromethane(125 ml) at 70° C. was added dropwise diisobutyl aluminum hydride intoluene (1.5M, 41.5 ml) for 10 minutes. The stirring was continued at-70° C. for 1 hour. To this cold mixture were added water (50 ml) andsaturated ammonium chloride (50 ml). The precipitate formed was filteredoff, and the remaining solution was extracted three times withdichloromethane. The organic layer was dried over magnesium sulfate.Evaporation of the solvent followed by column chromatography (silicagel, chloroform/methanol=20/1) gave Object Compound (1.44 g) as whitecrystals.

mp: 147-148° C.; MASS: 173 (M+H)⁺ ; NMR (CDCl₃, δ): 7.27 (1H, s), 7.37(1H, s), 7.58 (2H, d, J=8 Hz), 7.98 (1H, s), 8.03 (2H, d, J=8 Hz), 10.05(1H, s)

Preparation 95

A mixture of Starting Compound (7.72 g), iodomethane (5.47 g), andpotassium carbonate (6.34 g) in N,N-dimethylformamide (30 ml) was heatedat 60° C. for 3 hours. The mixture was evaporated, then diluted withwater, and extracted three times with ethyl acetate. The organic layerwas dried over magnesium sulfate. Evaporation of the solvent followed bycolumn chromatography (silica gel, hexane/ethyl acetate=3/2) gave ObjectCompound (8.14 g) as a yellow oil.

MASS (m/z): 267 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (2/5×3H, t, J=7 Hz), 1.44(3/5×3H, t, J=7 Hz), 1.82 (3/5×3H, s), 2.25 (2/5×3H, s), 3.22 (3/5×3H,s), 3.46 (2/5×3H, s), 4.42 (2/5×2H, q, J=7 Hz), 4.44 (3/5×2H, q, J=7Hz), 7.40 (2/5×1H, d, J=8 Hz), 7.48 (3/5×1H, d, J=8 Hz), 8.30 (2/5×1H,dd, J=8, 2 Hz), 8.34 (3/5×1H, dd, J=8, 2 Hz), 8.58 (2/5×1H, d, J=2 Hz),8.62 (3/5×1H, d, J=2 Hz)

Preparation 96

A mixture of Starting Compound (8.09 g) and powdered iron (17.0 g) inacetic acid-ethanol (1:1, 183 ml) was slowly heated until the reactionwas initiated (about 70° C.). The inner temperature rose to 89° C. Afterthe reaction subsided, the mixture was refluxed for 1 hour and allowedto cool to room temperature. The mixture was carefully poured into thesuspension of sodium carbonate (145 g) in water (600 ml). Theprecipitate formed was filtered, then the filtrate was made basic byadding 1N sodium hydroxide, extracted three times with ethyl acetate,washed once with brine, and dried over magnesium sulfate. Evaporation ofthe solvent gave crude product (5.74 g) as crystals. This wasrecrystallized from toluene (18 ml)--hexane (36 ml) to give ObjectCompound (5.55 g) of colorless crystals.

mp: 130-131° C.; MASS (m/z): 219 (M+H)⁺ ; NMR (CDCl₃, δ): 1.41 (3H, t,J=7 Hz), 2.60 (3H, s), 3.73 (3H, s), 4.29 (2H, q, J=7 Hz), 7.26 (1H, d,J=9 Hz), 7.98 (1H, d, J=9 Hz), 8.39 (1H, s)

Preparation 97

To an ice-cooled suspension of lithium aluminum hydride (950 mg) intetrahydrofuran (50 ml) was added Starting Compound (5.45 g), and themixture was stirred at room temperature for 1 hour. The mixture wascooled with ice and diluted with ether (100 ml). Then, water (0.95 ml),15% sodium hydroxide (0.95 ml), and water (1.9 ml) were added dropwiseto the mixture and filtered. To the precipitate was added ethanol, andthe insoluble matter was filtered off. The combined filtrate wasevaporated to give Object Compound (4.29 g) as white crystals.

mp: 162-164° C.; MASS (m/z): 177 (M+H)⁺ ; NMR (CDCl₃, δ): 2.57 (3H, s),3.69 (3H, s), 4.75 (2H, s), 7.25 (2H, ABq, Δ=0.05, J=8 Hz), 7.61 (1H, s)

Preparation 98

To a stirred solution of oxalyl chloride (5.85 g) in dichloromethane (23ml) below -60° C. was added dimethyl sulfoxide (4.50 g) dropwise. Tothis solution was added dropwise Starting Compound (4.05 g) in dimethylsuifoxide (20 ml)--dichloromethane (73 ml) with cooling below -55° C.The stirring was continued at -60° C. for 1 hour, then triethylamine(16.0 ml) was added dropwise, and the mixture was allowed to warm toroom temperature. Water (50 ml) was added thereto, then the mixture wasextracted four times with chloroform and dried over magnesium sulfate.Evaporation of the solvent followed by column chromatography (silicagel, chloroform/methanol 30/1) gave Object Compound (3.37 g) asoff-white crystals.

mp: 73-74° C.; MASS (m/z): 175 (M+H)⁺ ; NMR (CDCl₃, δ): 2.64 (3H, s),3.77 (3H, s), 7.37 (1H, d, J=8 Hz), 7.84 (1H, d, J=8 Hz), 8.16 (1H, s),10.06 (1H, s)

Preparation 99

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS: 530 (M+1); NMR (CDCl₃, δ): 1.40 (9H, s), 2.29 (3H, s), 2.52(3×2/3H, s), 2.80 (3×1/3H, s), 2.90-3.08 (4H, m), 4.02 (2×1/6H, d, J=16Hz), 4.22 (2×1/6H, d, J=16 Hz), 4.30 (2×1/3H, d, J=15 Hz), 4.58 (2×1/3H,d, J=15 Hz), 4.23-4.42 (1H, m), 4.83-4.95 (1H, m), 5.07-5.18 (1H, m),6.69 (1×1/3H, d, J=8 Hz), 6.80 (1×2/3H, d, J=8 Hz), 6.89 (1×2/3H, t, J=8Hz), 7.08 (1×1/3H, t, J=8 Hz), 7.00-7.14 (8H, m), 7.15-7.21 (2H, m),7.22-7.31 (3H, m)

(2) MASS: 528 (M+1); NMR (CDCl₃, δ): 1.30 (9×1/3H, s), 1.31 (9×2/3H, s),2.70-3.25 (8H, m), 4.40-5.09 (5H, m), 5.13-5.28 (1H, m), 6.82-7.48 (14H,m)

(3) MASS: 473 (M+1); NMR (CDCl₃, δ): 0.80 (3×1/5H, t, J=8 Hz), 0.85(3×4/5H, t, J=8 Hz), 1.18-1.40 (4H, m), 1.43 (9H, s), 1.57-1.82 (2H, m),2.97 (3×1/5H, s), 3.08 (3×4/5H, s), 3.58-3.68 (1H, m), 3.90-4.03 (2H,m), 4.20-4.31 (1H, m), 4.19 (2×2/5H, d, J=15 Hz), 4.21 (2×1/10H, d, J=16Hz), 4.84 (2×2/5H, d, J=15 Hz), 4.90 (2×1/10H, d, J=16 Hz), 4.86-5.00(1H, m), 5.52 (1H, d, J=7 Hz), 7.08-7.20 (1H, m), 7.57 (1H, q, J=8 Hz),7.70 (1H, t, J=8 Hz), 7.80 (1×4/5H, d, J=8 Hz), 7.83 (1×1/5H, d, J=8Hz), 8.00 (1×4/5H, s), 8.12 (1×1/5H, s), 8.10 (1H, d, J=8 Hz), 8.78(1×4/5H, s), 8.83 (1×1/5H, s)

(4) MASS: 534 (M+1); NMR (CDCl₃, δ): 0.73 (3×1/4H, t, J=8 Hz), 0.79(3×3/4H, t, J=8 Hz), 0.98-1.30 (4H, m), 1.32-1.62 (1H, m), 1.47 (9H, s),1.63-1.70 (1H, m), 2.92 (3×1/4H, s), 3.00 (3×3/4H, s), 3.19 (1×1/4H, s),3.22 (1×3/4H, s), 3.28-3.42 (1H, m), 4.52 (2×3/8H, d, J=15 Hz),4.53-4.63 (1H, m), 4.72 (2×1/8H, d, J=16 Hz), 4.87 (2×1/8H, d, J=16 Hz),4.92 (2×3/8H, d, J=15 Hz), 4.81-4.92 (1H, m), 6.50-6.60 (1H, m),7.10-7.21 (2H, m), 7.50-7.61 (3H, m), 7.70 (1H, t, J=8 Hz), 7.72-7.88(1H, m), 7.98 (1H, s), 8.09 (1×3/4H, d, J=8 Hz), 8.11 (1×1/4H, d, J=8Hz), 8.50 (1H, d, J=2 Hz), 8.78 (1H, s)

(5) MASS: 531 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 1.82-1.98 (1H, m),1.99-2.10 (1H, m), 2.09 (3H, s), 2.47-2.53 (2H, m), 2.58 (3×2/3H, s),2.75 (3×1/3H, s), 3.00 (2H, d, J=8 Hz), 3.90 (3×1/3H, s), 3.91 (3×2/3H,s), 4.20-4.30 (1H, m), 4.29 (2×1/2H, d, J=15 Hz), 4.49 (2×1/2H, d, J=15Hz), 5.02-5.27 (2H, m), 6.61 (1×1/3H, d, J=8 Hz), 6.67 (1×2/3H, d, J=8Hz), 7.00 (1H, d, J=8 Hz), 7.07-7.30 (5H, m), 7.32 (1H, dd, J=8, 2 Hz),7.82 (1×1/3H, d, J=2 Hz), 7.94 (1×2/3H, d, J=2 Hz)

(6) MASS: 517 (M+1); NMR (CDCl₃, δ): 0.80 (3×1/4H, t, J=8 Hz), 0.84(3×3/4H, t, J=8 Hz), 1.18-1.40 (4H, m), 1.43 (9H, s), 1.53-1.70 (1H, m),1.70-1.82 (1H, m), 1.86-1.99 (1H, m), 2.00-2.12 (1H, m), 2.08 (3H, s),2.50-2.60 (2H, m), 2.98 (3×1/4H, s), 3.09 (3×3/4H, s), 4.22-4.38 (1H,m), 4.63 (2×3/8H, d, J=15 Hz), 4.87 (2×3/8H, d, J=15 Hz), 4.92 (2×1/4H,s), 4.90-5.03 (1H, m), 5.14-5.28 (1H, m), 6.90-7.03 (1H, m), 7.56 (1H,q, J=8 Hz), 7.70 (1H, q, J=8 Hz), 7.80 (1H, q, J=8 Hz), 8.00 (1H, s),8.10 (1×3/4H, d, J=8 Hz), 8.11 (1×1/4H, d, J=8 Hz), 8.78-8.82 (1H, m)

(7) MASS: 523 (M+1); NMR (CDCl₃, δ): 0.78 (3×1/4H, t, J=8 Hz), 0.83(3×3/4H, t, J=8 Hz), 1.10-1.38 (4H, m), 1.40 (9H, s), 1.51-1.80 (2H, m),2.92-3.20 (3H, m), 2.98 (3×1/4H, s), 3.05 (3×3/4H, s), 4.37-4.49 (1H,m), 4.68-4.92 (3H, m), 6.78-6.88 (1H, m), 7.21-7.30 (1H, m), 7.49(1×3/4H, s), 7.52 (1×1/4H, s), 7.52-7.61 (1H, m), 7.71 (1H, t, J=8 Hz),7.79 (1×3/4H, d, J=8 Hz), 7.84 (1×1/4H, d, J=8 Hz), 8.00 (1H, s), 8.09(1×3/4H, d, J=8 Hz), 8.11 (1×1/4H, d, J=8 Hz), 8.79 (1×3/4H, s), 8.81(1×1/4H, s)

(8) MASS: 611 (M+1); NMR (CDCl₃, δ): 1.39 (3H, t, J=8 Hz), 1.43 (9H, s),2.29 (3H, s), 2.32-2.47 (4H, m), 2.50 (3×3/4H, s), 2.71 (3×1/4H, s),2.49-2.62 (1H, m), 2.95-3.29 (3H, m), 3.40-3.52 (2H, m), 3.53-3.64 (2H,m), 3.92 (2×1/8H, d, J=16 Hz), 4.18 (2×3/8H, d, J=15 Hz), 4.28 (2×1/8H,d, J=16 Hz), 4.50 (2×3/8H, d, J=15 Hz), 4.31 (2H, q, J=8 Hz), 4.45-4.58(1H, m), 5.00-5.22 (1H, m), 6.01 (1H, d, J=8 Hz), 6.53 (1×1/4H, d, J=8Hz), 6.63 (1×3/4H, d, J=8 Hz), 6.92 (1×1/4H, d, J=8 Hz), 7.20 (1×3/4H,d, J=8 Hz), 7.11-7.30 (5H, m), 7.40 (1×1/4H, d, J=8 Hz), 7.43 (1×3/4H,d, J=8 Hz), 7.78 (1×1/4H, s), 7.89 (1×3/4H, s)

(9) MASS: 567 (M+1); NMR (CDCl₃, δ): 1.48 (9H, s), 2.30 (3×3/4H, s),2.32 (3×1/4H, s), 2.48-2.62 (1H, m), 2.58 (3×3/4H, s), 2.80 (3×1/4H, s),2.88-3.09 (2H, m), 3.10-3.23 (1H, m), 3.38-3.49 (2H, m), 3.52-3.62 (2H,m), 3.63-3.76 (4H, m), 4.12 (2×1/8H, d, J=16 Hz), 4.30 (2×3/8H, d, J=5Hz), 4.56 (2×1/8H, d, J=16 Hz), 4.62 (2×3/8H, d, J=15 Hz), 4.48-4.62(1H, m), 5.02-5.13 (1H, m), 6.00 (1H, d, J=8 Hz), 6.83 (1×3/4H, m),6.98-7.03 (1×1/4H, m), 6.98-7.13 (5H, m), 7.18-7.32 (3H, m), 7.39(1×1/4H, d, J=8 Hz), 7.43 (1×3/4H, d, J=8 Hz)

(10) MASS: 505 (M+1); NMR (CDCl₃, δ): 0.83 (3×1/3H, t, J=8 Hz), 0.92(3×2/3H, t, J=8 Hz), 1.22-1.50 (2H, m), 1.43 (9H, s), 1.53-1.78 (1H, m),2.48-2.61 (1H, m), 2.90 (3×1/3H, s), 2.96 (3×2/3H, s), 3.11-3.23 (1H,m), 3.38-3.50 (2H, m), 3.53-3.61 (2H, m), 3.62-3.70 (4H, m), 4.40(2×1/3H, d, J=15 Hz), 4.47-4.59 (2H, m), 4.60 (2×1/3H, s), 4.72 (2×1/3H,d, J=15 Hz), 4.84-4.99 (1H, m), 6.07 (1H, d, J=8 Hz), 7.13-7.48 (6H, m)

(11) MASS: 613 (M+1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.28 (3H, s),2.32-2.50 (4H, m), 2.50-2.62 (1H, m), 2.51 (3H, s), 2.52 (3×3/4H, s),2.71 (3×1/4H, s), 2.93-3.30 (3H, m), 3.38-3.52 (2H, m), 3.54-3.65 (2H,m), 3.99 (2×1/8H, d, J=16 Hz), 4.19 (2×1/8H, d, J=16 Hz), 4.20 (2×3/8H,d, J=15 Hz), 4.51 (2×3/8H, d, J=15 Hz), 4.47-4.60 (1H, m), 5.01-5.20(1H, m), 5.95-6.00 (1H, m), 6.81-7.21 (7H, m), 7.39 (1×1/4H, d, J=8 Hz),7.41 (1×3/4H, d, J=8 Hz), 8.05 (1×1/4H, s), 8.20 (1×3/4H, s)

(12) MASS: 570 (M+1); NMR (CDCl₃, δ): 1.30 (3×1/4H, t, J=8 Hz), 1.36(3×3/4H, t, J=8 Hz), 1.17-1.40 (4H, m), 1.48 (9H, s), 1.57-1.86 (2H, m),2.58 (1H, dd, J=16, 4 Hz), 2.99 (3×1/4H, s), 3.04 (3×3/4H, s), 3.18 (1H,d, J=16 Hz), 3.38-3.50 (2H, m), 3.52-3.61 (2H, m), 3.62-3.78 (4H, m),4.50-4.69 (1H, m), 4.61 (2×1/2H, d, J=16 Hz), 4.80-5.03 1H, m), 4.96(2×1/2H, d, J=16 Hz), 6.09 (1H, d, J=8 Hz), 7.32-7.50 (1H, m), 7.58 (1H,q, J=8 Hz), 7.70 (1H, t, J=8 Hz), 7.78-7.84 (1H, m), 8.00 (1H, s),8.08-8.16 (1H, m), 8.80 (1H, d, J=2 Hz)

(13) MASS: 625 (M+1); NMR (CDCl₃, δ): 0.91 (3×1/5H, t, J=8 Hz), 0.92(3×4/5H, t, J=8 Hz), 1.43 (9H, s), 1.63-1.80 (2H, m), 2.30 (3H, s),2.32-2.50 (4H, m), 2.50-2.63 (1H, m), 2.53 (3×4/5H, s), 2.72 (3×1/5H,s), 2.93-3.13 (2H, m), 3.14-3.30 (1H, m), 3.40-3.52 (2H, m), 3.54-3.63(2H, m), 3.82 (2H, t, J=8 Hz), 3.97 (2×1/2H, d, J=15 Hz), 4.32 (2×1/2H,d, J=15 Hz), 4.48-4.60 (1H, m), 5.00-5.17 (1H, m), 6.01 (1H, d, J=8 Hz),6.40 (1×1/5H, d. J=8 Hz), 6.48 (1×4/5H, d, J=8 Hz), 6.93-7.03 (1H, m),7.08-7.30 (6H, m), 7.33-7.47 (1H, m)

(14) MASS: 584 (M+1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.50 (3×2/3H, s),2.50-2.60 (1H, m), 2.71 (3×1/3H, s), 2.92-3.03 (2H, m), 3.20 (1H, d,J=15 Hz), 3.38-3.50 (2H, m), 3.52-3.60 (2H, m), 3.60-3.73 (4H, m), 3.90(3×1/3H, s), 3.91 (3×2/3H, s), 4.20 (2×1/2H, d, J=15 Hz), 4.49 (2×1/2H,d, J=15 Hz), 4.50-4.60 (1H, m), 5.01-5.11 (1×2/3H, m), 5.12-5.23(1×1/3H, m), 6.01 (1H, d, J=8 Hz), 6.59 (1×1/3H, d, J=8 Hz), 6.64(1×2/3H, d, J=8 Hz), 7.10-7.22 (4H, m), 7.22-7.30 (2H, m), 7.38-7.48t1H, m), 7.79 (1×1/3H, d, J=2 Hz), 7.91 (1×2/3H, d, J=2 Hz)

Preparation 100

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8, 41 or 54.

(1) MASS: 430 (M+1); NMR (CDCl₃, δ): 2.30 (3H, s), 2.36-2.48 (1×1/3H,m), 2.50-2.60 (1×2/3H, m), 2.66 (3×2/3H, s), 2.82 (3×1/3H, s), 2.88-3.18(3H, m), 3.46 (1×1/3H, dd, J=12, 4 Hz), 3.57 (1×2/3H, dd, J=12, 4 Hz),4.30 (2×1/3H, d, J=15 Hz), 4.31 (2×1/6H, d, J=16 Hz), 4.40 (2×1/6H, d,J=16 Hz), 4.67 (2×1/3H, d, J=15 Hz), 5.19 (1H, q, J=12 Hz), 6.93-7.30(14H, m), 7.91 (1×1/3H, d, J=8 Hz), 8.00 (1×2/3H, d, J=8 Hz)

(2) MASS: 428 (M+1); NMR (CDCl₃, δ): 2.70-2.85 (2H, m), 2.99-3.25 (3H,m), 3.00 (3×1/3H, s), 3.05 (3×2/3H, s), 3.92-4.15 (1H, m), 4.41-5.07(3H, m), 5.30-5.40 (1H, m), 7.00-7.80 (14H, m)

(3) MASS: 373 (M+1); NMR (CDCl₃, δ): 0.81 (3×1/4H, t, J=8 Hz), 0.85(3×3/4H, t, J=8 Hz), 1.17-1.42 (4H, m), 1.59-1.88 (2H, m), 3.00 (3×1/4H,s), 3.07 (3×3/4H, s), 3.41 (1×1/4H, t, J=5 Hz), 3.50 (1×3/4H, t, J=5Hz), 3.60-3.75 (1H, m), 3.80-3.90 (1H, m), 4.63 (2×1/8H, d, J=16 Hz),4.70 (2×3/8H, d, J=15 Hz), 4.81 (2×1/8H, d, J=16 Hz), 4.90 (2×3/8H, d,J=15 Hz), 4.81-5.07 (1H, m), 7.59 (1H, q, J=8 Hz), 7.68-7.90 (3H, m),8.01 (1×3/4H, s), 8.12 (1×1/4H, s), 8.10 (1H, d, J=8 Hz), 8.80 (1×3/4H,s), 8.82 (1×1/4H, s)

(4) MASS: 434 (M+1); NMR (CDCl₃, δ): 0.79 (3×1/3H, t, J=8 Hz), 0.87(3×2/3H, t, J=8 Hz), 1.10-1.35 (4H, m), 1.50-1.80 (2H, m), 2.98 (3×1/3H,s), 3.04 (3×2/3H, s), 3.00-3.12 (1H, m), 3.22-3.37 (1H, m), 3.63-3.71(1×1/3H, m), 3.75-3.85 (1×2/3H, m), 4.61 (2×1/3H, d, J=15 Hz), 4.83(2×1/6H, d, J=16 Hz), 4.92 (2×1/3H, d, J=15 Hz), 4.98 (2×1/6H, d, J=16Hz), 4.90-5.05 (1H, m), 7.11-7.30 (2H, m), 7.51-7.66 (2H, m), 7.71 (1H,t, J=8 Hz), 7.80 (1H, d, J=8 Hz), 8.01 (1H, s), 8.10 (1×2/3H, d, J=8Hz), 8.12 (1×1/3H, d, J=8 Hz), 8.20 (1×1/3H, d, J=8 Hz), 8.22 (1×2/3H,d, J=8 Hz), 8.50-8.58 (1H, m), 8.81 (1H, d, J=2 Hz)

(5) MASS: 431 (M+1); NMR (CDCl₃, δ): 1.62-1.79 (1H, m), 1.97-2.11 (1H,m), 2.09 (3×1/4H, s), 2.10 (3×3/4H, s), 2.48 (2×1/4H, t, J=8 Hz), 2.51(2×3/4H, t, J=8 Hz), 2.68 (3×3/4H, s), 2.78 (3×1/4H, s), 2.90-3.18 (2H,m), 3.40-3.51 (1H, m), 3.90 (3×1/4H, s), 3.91 (3×3/4H, s), 4.11 (2×1/8H,d, J=16 Hz), 4.24 (2×3/8H, d, J=15 Hz), 4.33 (2×3/8H, d, J=15 Hz), 4.57(2×1/8H, d, J=16 Hz), 5.08-5.18 (1×3/4H, m), 5.20-5.30 (1×1/4H, m), 6.62(1×1/4H, d, J=8 Hz), 6.68 (1×3/4H, d, J=8 Hz), 7.10-7.37 (6H, m), 7.88(1×1/4H, d, J=2 Hz), 7.90 (1H, d, J=8 Hz), 7.94 (1×3/4H, d, J=2 Hz)

(6) MASS: 417 (M+1); NMR (CDCl₃, δ): 0.80 (3×1/4H, t, J=8 Hz), 0.84(3×3/4H, t, J=8 Hz), 1.17-1.47 (4H, m), 1.50-1.90 (3H, m), 2.08-2.22(1H, m), 2.09 (3×1/4H, s), 2.10 (3×3/4H, s), 2.60 (2×1/4H, t, J=8 Hz),2.62 (2×3/4H, t, J=8 Hz), 3.00 (3×1/4H, s), 3.07 (3×3/4H, s), 3.40-3.48(1×1/4H, m), 3.50-3.58 (1×3/4H, m), 4.62 (2×1/2H, d, J=15 Hz), 4.92(2×1/2H, d, J=15 Hz), 4.80-5.06 (1H, m), 7.53 (1×3/4H, t, J=8 Hz), 7.57(1×1/4H, t, J=8 Hz), 7.70 (1H, t, J=8 Hz), 7.79 (1H, d, J=7 Hz), 7.90(1H, d, J=8 Hz), 8.01 (1H, s), 8.09 (1×3/4H, d, J=7 Hz), 8.11 (1×1/4H,d, J=7 Hz), 8.81 (1H, d, J=2 Hz)

(7) MASS: 423 (M+1); NMR (CDCl₃, δ): 0.79 (3×1/4H, t, J=8 Hz), 0.87(3×3/4H, t, J=8 Hz), 1.00-1.40 (4H, m), 2.53-2.80 (2H, m), 2.90-3.06(2H, m), 2.98 (3×1/4H, s), 3.04 (3×3/4H, s), 3.49-3.58 (1×1/4H, m),3.60-3.70 (1×3/4H, m), 4.78 (2×3/4H, s), 4.81-4.93 (2×1/4H, s),4.81-5.02 (1H, m), 6.86 (1H, s), 7.50-7.60 (2H, m), 7.71 (1H, t, J=8Hz), 7.79 (1H, q, J=8 Hz), 7.90 (1×3/4H, d, J=8 Hz), 7.93 (1×1/4H, d,J=8 Hz), 8.00 (1×3/4H, s), 8.03 (1×1/4H, s), 8.09 (1×3/4H, d, J=8 Hz),8.11 (1×1/4H, d, J=8 Hz), 8.79 (1×3/4H, s), 8.81 (1×1/4H, s)

(8) MASS: 511 (M+1); NMR (CDCl₃, δ): 1.38 (3H, t, J=8 Hz), 2.29 (3H, s),2.32-2.52 (5H, m), 2.61 (3×3/4H, s), 2.77 (3×1/4H, s), 2.70-2.88 (1H,m), 2.93-3.18 (2H, m), 3.37-3.48 (2H, m), 3.51-3.74 (3H, m), 4.11(2×1/8H, d, J=16 Hz), 4.20 (2×3/8H, d, J=15 Hz), 4.32 (2×1/8H, d, J=16Hz), 4.53 (2×3/8H, d, J=15 Hz), 4.29 (2H, q, J=8 Hz), 5.11 (1×3/4H, q,J=8 Hz), 5.20 (1×1/4H, q, J=8 Hz), 6.59 (1×1/4H, d, J=8 Hz), 6.62(1×3/4H, d, J=8 Hz), 7.07 (1×1/4H, d, J=8 Hz), 7.18 (1×3/4H, d, J=8 Hz),7.10-7.32 (5H, m), 7.81 (1×1/4H, s), 7.91 (1×3/4H, s), 8.12 (1×1/4H, d,J=8 Hz), 8.16 (1×3/4H, d, J=8 Hz)

(9) MASS: 467 (M+1); NMR (CDCl₃, δ): 2.28 (3H, s), 2.33-2.58 (1H, m),2.68 (3×2/3H, s), 2.80 (1H, dd, J=17, 2 Hz), 2.83 (3×1/3H, s), 2.90-3.10(2H, m), 3.33-3.48 (2H, m), 3.50-3.78 (7H, m), 4.32 (2×1/3H, d, J=15Hz), 4.38 (2×1/3H, s), 4.69 (2×1/3H, d, J=15 Hz), 5.08-5.20 (1H, m),6.93-7.13 (6H, m), 7.20-7.32 (3H, m), 8.03 (1×1/3H, d, J=8 Hz), 8.11(1×2/3H, d, J=8 Hz)

(10) MASS: 405 (M+1); NMR (CDCl₃, δ): 0.87 (3×1/3H, t, J=8 Hz), 0.93(3×2/3H, t, J=8 Hz), 1.22-1.50 (2H, m), 1.58-1.80 (2H, m), 2.58-2.72(1H, m), 2.80-2.91 (1H, m), 2.92 (3×1/3H, s), 3.01 (3×2/3H, s),3.40-3.51 (2H, m ), 3.52-3.71 (6H, m), 3.72-3.80 (1H, m), 4.46 (2×1/3H,d, J=15 Hz), 4.67 (2×1/3H, s), 4.77 (2×1/3H, d, J=15 Hz), 4.88-5.00 (1H,m), 7.17-7.42 (5H, m), 8.08 (1×1/3H, d, J=8 Hz), 8.12 (1×2/3H, d, J=8Hz)

(11) MASS: 513 (M+1); NMR (CDCl₃, δ): 2.32 (3H, s), 2.38-2.52 (6H, m),2.52 (3×1/3H, s), 2.53 (3×2/3H, s), 2.64 (3×2/3H, s), 2.79 (3×1/3H, s),2.73-2.88 (1H, m), 2.93-3.20 (1H, m), 3.42-3.51 (2H, m), 3.53-3.78 (3H,m), 4.18 (2×1/6H, d, J=16 Hz), 4.28 (2×1/3H, d, J=15 Hz), 4.31 (2×1/6H,d, J=16 Hz), 4.55 (2×1/3H, d, J=15 Hz), 5.07-5.21 (1H, m), 6.97-7.32(7H, m), 8.12 (1H, s), 8.16 (1×1/3H, s), 8.22 (1×2/3H, s)

(12) MASS: 470 (M+1); NMR (CDCl₃, δ): 0.80 (3×1/5H, t, J=8 Hz), 0.85(3×4/5H, t, J=8 Hz), 1.15-1.40 (4H, m), 1.60-1.90 (2H, m), 2.63 (1×1/5H,d, J=8 Hz), 2.70 (1×4/5H, d, J=8 Hz), 2.80 (1H, t, J=15 Hz), 2.99(3×1/5H, s), 3.03 (3×4/5H, s), 3.40-3.50 (2H, m), 3.50-3.70 (6H, m),3.70-3.80 (1H, m), 4.63 (2×1/2H, d, J=15 Hz), 4.80-5.02 (1H, m), 4.90(2×1/2H, d, J=15 Hz), 7.50-7.60 (1H, m), 7.71 (1H, t, J=8 Hz), 7.80 (1H,d, J=8 Hz), 8.01 (1H, s), 8.10 (2×4/5H, d, J=8 Hz), 8.12 (2×1/5H, d, J=8Hz), 8.80 (1H, d, J=8 Hz)

(13) MASS: 525 (M+1); NMR (CDC₃, δ): 0.90 (3×1/5H, t, J=8 Hz), 0.92(3×4/5H, t, J=8 Hz), 1.67-1.90 (2H, m), 2.29 (3H, s), 2.33-2.48 (4H, m),2.49-2.60 (1H, m), 2.61 (3×4/5H, s), 2.76 (3×1/5H, s), 2.72-2.88 (1H,m), 2.92-3.09 (2H, m), 3.40-3.50 (2H, m), 3.51-3.72 (3H, m), 3.79(2×1/10H, d, J=16 Hz), 3.85 (2H, t, J=8 Hz), 3.99 (2×2/5H, d, J=15 Hz),4.08 (2×1/10H, d, J=16 Hz), 4.39 (2×2/5H, d, J=15 Hz), 5.01-5.20 (1H,m), 6.41 (1×1/5H, d, J=8 Hz), 6.49 (1×4/5H, d, J=8 Hz), 6.81 (1×1/5H, d,J=8 Hz), 7.03 (1×4/5H, d, J=8 Hz), 7.10-7.32 (6H, m), 8.15 (1H, d, J=8Hz)

(14) MASS: 484 (M+1); NMR (CDCl₃, δ): 2.40-2.58 (1H, m), 2.63 (3×3/4H,s), 2.70-2.82 (1H, m), 2.78 (3×1/4H, s), 2.93-3.18 (2H, m), 3.38-3.50(2H, m), 3.51-3.74 (7H, m), 3.90 (3×1/4H, s), 3.91 (3×3/4H, s), 4.10(2×1/8H, d, J=16 Hz), 4.23 (2×3/8H, d, J=15 Hz), 4.31 (2×1/8H, d, J=16Hz), 4.56 (2×3/8H, d, J=15 Hz), 5.04-5.27 (1H, m), 6.61 (1×1/4H, d, J=8Hz), 6.68 (1×3/4H, d, J=8 Hz), 7.03-7.36 (6H, m), 7.84 (1×1/4H, s), 7.93(1×3/4H, s), 8.11 (1×1/4H, d, J=8 Hz), 8.13 (1×3/4H, d, J=8 Hz)

Preparation 101

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS: 414 (M+1); NMR (CDCl₃, δ): 1.35 (3H, t, J=8 Hz), 1.39 (9H, s),2.58 (3×3/4H, s), 2.77 (3×1/4H, s), 2.90-3.10 (2H, m), 3.90 (2×1/8H, d,J=16 Hz), 4.26 (2×1/8H, d, J=16 Hz), 4.31 (2H q, J=8 Hz), 4.33 (2×3/8H,d, J=15 Hz), 4.43 (2×3/8H, d, J=15 Hz), 4.73-4.88 (1×2/3H, m) 4.90-5.00(1×1/3H, m), 5.30-5.43 (1H, m), 6.59 (1×1/4H, d, J=8 Hz), 6.63 (1×3/4H,d, J=8 Hz), 7.02-7.36 (6H, m), 7.81 (1×1/4H, s), 7.92 (1×3/4H, s)

(2) MASS: 383 (M+1); NMR (CDCl₃, δ): 1.40 (9×1/3H, s), 1-42 (9×2/3H, s),2.28 (3×2/3H, s), 2.30 (3×1/3H, s), 2.61 (3×2/3H, s), 2.81 (3×1/3H, s),2.87-3.00 (2H, m), 4.14 (2×1/6H, d, J=16 Hz), 4.37 (2×1/6H, d, J=16 Hz),4.42 (2×1/3H, d, J=15 Hz), 4.56 (2×1/3H, d, J=15 Hz), 4.79-4.92 (1H, m),5.32 (1×1/3H, d, J=8 Hz), 5.40 (1×2/3H, d, J=8 Hz), 6.91-7.18 (6H, m),7.20-7.31 (3H, m)

(3) MASS: 321 (M+1); NMR (CDCl₃, δ): 0.83 (3×1/3H, t, J=8 Hz), 0.90(3×2/3H, t, J=8 Hz), 1.20-1.78 (4H, m), 1.41 (9×1/3H, s), 1.43 (9×2/3H,s), 2.90 (3×1/3H, s), 2.94 (3×2/3H, s), 4.51 (2×1/2H, d, J=15Hz), 4.68(2×1/2H, d, J=15 Hz), 4.59-4.73 (1H, m), 5.31 (1×1/3H, d, J=8 Hz), 5.39(1×2/3H, d, J=8 Hz), 7.12-7.40 (5H, m)

(4) MASS: 416 (M+1); NMR (CDCl₃, δ): 1.40 (9H, s), 2.51 (3×1/5H, s),2.53 (3×4/5H, s), 2.58 (3×1/5H, s), 2.76 (3×4/5H, s), 2.90-3.07 (2H, m),3.97 (2×1/10H, d, J=16 Hz), 4.29 (2×1/10H, d, J=16 Hz), 4.32 (2×2/5H, d,J=15 Hz), 4.42 (2×2/5H, d, J=15 Hz), 4.77-4.97 (1H, m), 5.29-5.40 (1H,m), 6.93-7.30 (7H, m), 8.10 (1×1/5H, s), 8.21 (1×4/5H, s)

(5) MASS: 386 (M+1); NMR (CDCl₃, δ): 0.80 (3×1/4H, t, J=8 Hz), 0.88(3×3/4H, t, J=8 Hz), 1.18-1.38 (3H, m), 1.39 (9×1/4H, s), 1.41 (9×3/4H,s), 1.51-1.63 (1H, m), 1.64-1.73 (2H, m), 2.99 (3×1/4H, s), 3.08(3×3/4H, s), 4.60-4.69 (1H, m), 4.70 (2×3/8H, d, J=15 Hz), 4.78 (2×1/8H,d, J=17 Hz), 4.87 (2×3/8H, d, J=15 Hz), 4.89 (2×1/8H, d, J=17 Hz), 5.29(1×1/4H, d, J=8 Hz), 5.33 (1×3/4H, d, J=8 Hz), 7.53 (1H, t, J=8 Hz),7.70 (1H, t, J=8 Hz), 7.79 (1H, d, J=8 Hz), 8.00 (1H, s), 8.09 (1H, d,J=8 Hz), 8.81 (1H, d, J=2 Hz)

(6) MASS: 428 (M+1); NMR (CDCl₃, δ): 0.90 (3×1/5H, t, J=8 Hz), 0.93(3×4/5H, t, J=8 Hz), 1.39 (9H, s), 1.65-1.82 (2H, m), 2.60 (3×4/5H, s),2.75 (3×1/5H, s), 2.90-3.03 (2H, m), 3.51 (2×1/10H, d, J=16 Hz),3.77-3.90 (2H, m), 4.10 (2×1/10H, d, J=16 Hz), 4.11 (2×2/5H, d, J=15Hz), 4.22 (2×2/5H, d, J=15 Hz), 4.73-5.92 (1H, m), 5.32 (1H, d, J=8 Hz),6.43 (1×1/5H, d, J=8 Hz), 6.49 (1×4/5H, d, J=8 Hz), 6.85 (1×1/5H, dd,J=12, 3 Hz), 7.10 (1×4/5H, dd, J=12, 3 Hz), 7.02-7.32 (6H, m)

(7) MASS: 381 (M+1); NMR (CDCl₃, δ): 1.35 (9×2/9H, s), 1.39 (9×2/9H, s),1.49 (9×5/9H, s), 2.83-3.20 (2H, m), 3.03 (3H, s), 4.33-4.71 (2H, m),4.73-5.00 (2H, m), 5.21-5.38 (1H, m), 7.08-7.45 (9H, m)

Preparation 102

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8, 41 or 54.

(1) MASS: 314 (M+1); NMR (CDCl₃, δ): 1.39 (3H, t, J=8 Hz), 2.62 (3×3/4H,s), 2.88 (3×1/4H, s), 2.72-2.88 (1H, m), 2.88-3.08 (1H, m), 3.88-4.00(1H, m), 4.03 (2×1/8H, d, J=16 Hz), 4.30 (2×1/8H, d, J=16 Hz), 4.32(2×3/8H, d, J=15 Hz), 4.32 (2H, q, J=8 Hz), 4.53 (2×3/8H, d, J=15 Hz),6.63 (1×1/4H, d, J=8 Hz), 6.67 (1×3/4H, d, J=1 Hz), 7.10-7.32 (5H, m),7.41 (1H, dd, J=8, 2 Hz), 7.88 (1×1/4H, s), 7.97 (1×3/4H, s)

(2) MASS: 283 (M+1); NMR (CDCl₃, δ): 2.28 (3H, s), 2.63-2.80 (1H, m),2.71 (3×2/3H, s), 2.90 (3×1/3H, s), 2.88-3.00 (1H, m), 3.86 (1×1/3H, t,J=8 Hz), 3.97 (1×2/3H, t, J=8 Hz), 4.20 (2×1/6H, d, J=16 Hz), 4.40(2×1/6H, d, J=16 Hz), 4.45 (2×1/3H, d, J=15 Hz), 4.63 (2×1/3H, d, J=15Hz), 6.97-7.18 (6H, m) 7.20-7.38 (3H, m)

(3) MASS: 221 (M+1); NMR (CDCl₃, δ): 0.82-100 (3H, m), 1.30-1.70 (4H,m), 2.91 (3×2/3H, s), 2.94 (3×1/3H, s), 3.63-3.82 (1H, m), 4.46 (2×1/6H,d, J=16 Hz), 4.50 (2×1/3H, d, J=15 Hz), 4.68 (2×1/6H, d, J=16 Hz), 4.71(2×1/3H, d, J=15 Hz), 7.13-7.41 (5H, m)

(4) MASS: 316 (M+1); NMR (CDCl₃, δ): 2.55 (3H, s), 2.59 (3×3/4H, s),2.73-2.89 (1H, m), 2.88 (3×1/4H, s), 2.90-3.08 (1H, m), 3.87-4.00 (1H,m), 4.09 (2×1/8H, d, J=16 Hz), 4.31 (2×1/8H, d, J=16 Hz), 4.37 (2×3/8H,d, J=15 Hz), 4.57 (2×3/8H, d, J=15 Hz), 7.02-7.35 (7H, m), 8.18 (1×1/4H,s), 8.27 (1×3/4H, s)

(5) MASS: 286 (M+1); NMR (CDCl₃, δ): 0.9 0 (3H, t, J=8 Hz), 1.20-1.58(6H, m), 3.00 (3H, s), 3.72 (1H, d, J=8 Hz), 4.68 (2×3/8H, d, J=15 Hz),4.71 (2×1/8H, d, J=16 Hz), 4.83 (2×1/8H, d, J=16 Hz), 4.91 (2×3/8H, d,J=15 Hz), 7.53 (1H, t, J=8 Hz), 7.70 (1H, t, J=8 Hz), 7.80 (1H, d, J=8Hz), 7.92 (1×1/4H, s), 8.01 (1×3/4H, s), 8.09 (1H, d, J=8 Hz), 8.80 (1H,s)

(6) MASS: 328 (M+1); NMR (CDCl₃, δ): 0.98 (3H, t, J=8 Hz), 1.70-1.84(2H, m), 2.63 (3×3/4H, s), 2.81 (3×1/4H, s), 2.74-2.89 (1H, m),2.90-3.00 (1H, m), 3.88 (2H, t, J=8 Hz), 3.92 (1H, t, J=8 Hz), 4.10(2×1/2H, d, J=15 Hz), 4.38 (2×1/2H, d, J=8 Hz), 6.51 (1H, d, J=8 Hz),7.10-7.21 (4H, m), 7.21-7.35 (3H, m)

(7) MASS: 281 (M+1); NMR (CDCl₃, δ): 2.70-2.91 (1H, m), 2.92-3.17 (1H,m), 2.99 (3×1/2H, s), 3.00 (3×1/2H, s), 3.88-4.18 (3H, m), 4.60 (2×1/3H,d, J=17 Hz), 4.66 (2×1/3H, s), 4.78 (2×1/3H, d, J=17 Hz), 6.98-7.40 (9H,m)

Preparation 103

The following object compounds were obtained according to a similarmanner to that of Preparation 22, 23, 25, 67 or 68.

(1) MASS: 167 (M+1); NMR (CDCl₃, δ): 1.32 (3H, t, J=8 Hz), 2.42 (3H, s),3.62 (2H, s), 4.31 (2H, q, J=8 Hz), 6.69 (1H, d, J=8 Hz), 7.57 (1H, dd,J=8, 2 Hz), 8.03 (1H, d, J=2 Hz)

(2) MASS: 169 (M+1); NMR (CDCl₃, δ): 2.43 (3H, s), 2.57 (3H, s), 3.68(2H, s), 7.16 (1H, d, J=8 Hz), 7.49 (1H, dd, J=8, 3 Hz), 8.37 (1H, s)

(3) MASS: 181 (M+1); NMR (CDCl₃, δ): 1.43 (3H, t, J=8 Hz), 1.70-1.84(2H, m), 2.39 (3H, s), 3.50 (2H, s), 3.89 (2H, t, J=8 Hz), 6.52 (1H, d,J=8 Hz), 7.20 (1H, d, J=2 Hz), 7.30 (1H, dd, J=8, 2 Hz)

Preparation 104

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS: 413 (M+1); NMR (CDCl₃, δ): 0.85 (3×1/6H, t, J=8 Hz), 0.90(3×5/6H, t, J=8 Hz), 1.20-1.40 (4H, m), 1.41 (9×1/6H, s), 1.42 (9×5/6H,s), 1.50-1.78 (2H, m), 2.96 (3×1/6H, s), 3.09 (3×5/6H, s), 4.58-4.81(3H, m), 5.29 (1×1/6H, d, J=8 Hz), 5.32 (1×5/6H, d, J=8 Hz), 7.37-7.43(1H, m), 7.68-7.80 (2H, m), 8.30 (1H, d, J=8 Hz), 8.60 (1H, s), 8.65(1H, d, J=2 Hz), 9.20 (1H, s)

(2) MASS (m/z): 350 (M⁺ +1); NMR (CDCl₃, δ): 0.89 (3H, m), 1.33 (4H, m),1.54-1.67 (2H, m), 2.55 (3H, s), 2.89 (3H×1/4, s), 3.01 (3H×3/4, s),4.46-4.66 (3H, m), 5.33 (1H, m), 7.12 (1H, d, J=8 Hz), 7.47 (1H, dd,J=2, 8 Hz), 8.37 (1H, d, J=2 Hz)

(3) MASS: 400 (M+1); NMR (CDCl₃, δ): 1.38 (9×1/4H, s), 1.39 (9×3/4H, s),2.61 (3×3/4H, s), 2.79 (3×1/4H, s), 2.99 (2×3/4H, d, J=8 Hz), 3.01(2×1/4H, d, J=8 Hz), 3.80 (3×1.4H, s), 3.81 (3×3/4H, s), 3.78 (2×1/8H,d, J=16 Hz), 4.38 (2×1/8H, d, J=16 Hz), 4.41 (2×3/8H, d, J=15 Hz), 4.52(2×3/8H, d, J=15 Hz), 4.82 (1×3/4H, q, J=8 Hz), 4.93 (1×1/4H, q, J=8Hz), 5.29-5.40 (1H, m), 7.01 (1×1/4H, s), 7.08 (1×3/4H, s), 7.10-7.32(5H, m), 7.89 (1×1/4H, s), 8.01 (1×3/4H, s), 8.21 (1×1/4H, s), 8.23(1×3/4H, s)

(4) MASS: 400 (M+1); NMR (CDCl₃, δ): 1.41 (9H, s), 2.65 (3×2/3H, s),2.71 (3×1/3H, s), 2.90-3.10 (2H, m), 3.50 (2×1/6H, d, J=16 Hz), 3.80(3×1/3H, s), 3.82 (3×2/3H, s), 4.40 (2×1/6H, d, J=16 Hz), 4.42 (2×1/3H,d, J=15 Hz), 4.58 (2×1/3H, d, J=15 Hz), 4.83 (1×2/3H, m), 5.16 (1×1/3H,m), 5.40 (1×2/3H, d, J=8 Hz), 5.52 (1×1/3H, d, J=8 Hz), 6.72 (1×1/3H, d,J=6 Hz), 6.76 (1×2/3H, d, J=6 Hz), 7.09-7.32 (5H, m), 8.06 (1×1/3H, s),8.23 (1×2/3H, s), 8.42 (1H, d, J=6 Hz)

(5) MASS: 448 (M+1); NMR (CDCl₃, δ): 1.41 (9×1/6H, s), 1.42 (9×5/6H, s),2.61 (3×5/6H, s), 2.79 (3×1/6H, s), 2.91-3.10 (2H, m), 3.91 (2×1/12H, d,J=16 Hz), 4.38 (2×1/12H, d, J=16 Hz), 4.41 (2×5/12H, d, J=15 Hz), 4.50(2×5/12H, d, J=15 Hz), 4.78-4.93 (1H, m), 5.28-5.41 (1H, m), 7.11-7.31(5H, m), 7.51 (1×1/6H, s), 7.69 (1×5/6H, s), 8.18 (1×1/6H, s), 8.31(1×5/6H, s), 8.61 (1H, s)

Preparation 105

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8, 41 or 54.

(1) MASS: 313 (M+1); NMR (CDCl₃, δ): 0.90 (3H, t, J=8 Hz), 1.20-1.58(4H, m), 1.59-1.80 (2H, m), 3.00 (3H, s), 3.62-3.78 (1H, m), 4.57(2×1/2H, d, J=15 Hz), 4.74 (2×1/2H, d, J=15 Hz), 7.35-7.44 (1H, m),7.60-7.80 (2H, m), 8.30 (1H, d, J=8 Hz), 8.60 (1H, s), 8.66 (1H, d, J=3Hz), 9.19 (1H, s)

(2) NMR (CDCl₃, δ): 0.92 (3H, t, J=7 Hz), 1.31-1.58 (6H, m), 2.54 (3H,s), 2.94 (3H, s), 3.68 (1H, m), 4.45 (1H, d, J=15 Hz), 4.67 (1H, d, J=15Hz), 7.13 (1H, d, J=8 Hz), 7.50 (1H, dd, J=2, 8 Hz), 8.37 (1H, d, J=2Hz)

(3) MASS: 300 (M+1); NMR (CDCl₃, δ): 2.70 (3×3/4H, s), 2.73-2.87 (1H,m), 2.90 (3×1/4H, s), 2.93-3.07 (1H, m), 3.82 (3×1/4H, s), 3.86 (3×3/4H,s), 3.88 (1×1/4H, s), 3.96 (1×3/4H, s), 4.12 (2×1/6H, d, J=16 Hz), 4.40(2×1/6H, d, J=15 Hz), 4.48 (2×1/3H, d, J=15 Hz), 4.60 (2×1/3H, d, J=15Hz), 6.91 (1×1/4H, s), 7.11 (1×3/4H, s), 7.09-7.33 (5H, m), 7.98(1×1/4H, s), 8.07 (1×3/4H, s), 8.23 (1H, d, J=2 Hz)

(4) MASS: 300 (M+1); NMR (CDCl₃, δ): 2.38-2.45 (1H, m), 2.45-2.52 (1H,m), 2.41 (3×2/3H, s), 2.43 (3×1/3H, s), 3.93 (3H, s), 3.94-4.03 (1H, m),3.98 (2×1/6H, d, J=16 Hz), 4.22 (2×1/6H, d, J=16 Hz), 4.23 (2×1/3H, d,J=15 Hz), 4.33 (2×1/3H, d, J=15 Hz), 6.38-6.41 (1H, m), 6.66-6.70 (5H,m), 8.07 (1×1/3H, s), 8.13 (1×2/3H, s), 8.20-8.27 (1H, m)

(5) MASS: 348 (M+1); NMR (CDCl₃, δ): 2.68 (3×5/6H, s), 2.85 (3×1/6H, s),2.78-2.90 (1H, m), 2.92-3.08 (1H, m), 3.83 (1×1/6H, t, J=8 Hz), 3.97(1×5/6H, t, J=8 Hz), 4.11 (2×1/12H, d, J=16 Hz), 4.38 (2×1/12H, d, J=16Hz), 4.39 (2×5/12H, d, J=15 Hz), 4.61 (2×5/12H, d, J=15 Hz), 7.10-7.35(5H, m), 7.50 (1×1/6H, s), 7.71 (1×5/6H, s), 8.26 (1×1/6H, s), 8.38(1×5/6H, s), 8.60 (1H, d, J=2 Hz)

Preparation 106

The following object compounds were obtained according to a similarmanner to that of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS: 597 (M+1); NMR (CDCl₃, δ): 0.85 (3×1/4H, t, J=8 Hz), 0.89(3×3/4H, t, J=8 Hz), 1.20-1.41 (4H, m), 1.47 (9H, s), 1.58-1.85 (2H, m),2.57 (1H, dd, J=17, 4 Hz), 2.92 (3×1/4H, s), 3.04 (3×3/4H, s), 3.19 (1H,dd, J=17, 2 Hz), 3.40-3.50 (2H, m), 3.52-3.61 (2H, m), 3.62-3.85 (4H,m), 4.50-4.60 (1H, m), 4.57 (2×1/2H, d, J=15 Hz), 4.71 (2×1/2H, d, J=15Hz), 4.83-5.00 (1H, m), 6.08 (1H, d, J=8 Hz), 7.30-7.50 (2H, m),7.65-7.81 (2H, m), 8.31 (1H, d, J=8 Hz), 8.59 (1H, s), 8.67 (1H, d, J=2Hz), 9.20 (1H, s)

(2) MASS: 561 (M+1); NMR (CDCl₃, δ): 0.79 (3×1/4H, t, J=8 Hz), 0.80(3×3/4H, t, J=8 Hz), 0.93-1.30 (4H, m), 1.30-1.52 (1H, m), 1.43 (9H, s),1.52-1.70 (1H, m), 2.90 (3×1/4H, s), 3.01 (3×3/4H, s), 3.19 (1×1/4H, d,J=5 Hz), 3.21 (1×3/4H, d, J=5 Hz), 3.28-3.40 (1H, m), 4.51 (2×1/2H, d,J=15 Hz), 4.51-4.62 (1H, m), 4.69 (2×1/2H, d, J=15 Hz), 5.80-5.93 (1H,m), 6.50-6.60 (1H, m), 7.10-7.22 (2H, m), 7.37-7.45 (1H, m), 7.46-7.80(4H, m), 8.31 (1H, d, J=7 Hz), 8.51 (1H, d, J=4 Hz), 8.58 (1H, s), 8.65(1H, d, J=2 Hz), 9.19 (1H, s)

(3) MASS: 544 (M+1); NMR (CDCl₃, δ): 0.86 (3×1/5H, t, J=8 Hz), 0.90(3×4/5H, t, J=8 Hz), 1.29 (4×1/5H, t, J=8 Hz), 1.31 (4×4/5H, t, J=8 Hz),1.42 (9H, s), 1.55-1.70 (1H, m), 1.70-1.85 (1H, m), 1.87-2.18 (2H, m),2.09 (3H, s), 2.58 (2H, t, J=8 Hz), 2.94 (3×1/5H, s), 3.09 (3×4/5H, s),4.22-4.35 (1H, m), 4.59 (2×1/2H, d, J=15 Hz), 4.70 (2×1/2H, d, J=15 Hz),4.88-5.02 (1H, m), 5.12-5.23 (1H, m), 6.83-6.98 (1H, m), 7.41 (1H, dd,J=8, 6 Hz), 7.67-7.81 (2H, m), 8.30 (1H, d, J=8 Hz), 8.59 (1H, s), 8.66(1H, d, J=2 Hz), 9.19 (1H, s)

(4) MASS (m/z): 534 (M⁺ +1); NMR (CDCl₃, δ): 0.87 (3H, t, J=7 Hz), 1.31(4H, m), 1.47 (9H, s), 1.60-1.75 (2H, m), 2.54 (3H, s), 2.87 (3H×1/4,s), 2.98 (3H×3/4, s), 3.17 (1H, m), 3.43-3.57 (5H, m), 3.65 (4H, m),4.40 (1H×3/4, d, J=15 Hz), 4.53 (1H, m), 4.68 (2H×1/4, s), 4.67 (1H×3/4,d, J=15 Hz), 4.87 (1H, m), 6.06 (1H, d, J=7 Hz), 7.11-7.17 (1H, m),7.32-7.47 (2H, m), 8.35 (1H, m)

(5) MASS (m/z): 498 (M⁺ +1); NMR (CDCl₃, δ): 0.80 (3H, t, J=7 Hz), 1.03(2H, m), 1.17 (2H, m), 1.40 (1H, m), 1.46 (9H, s), 1.57 (1H, m), 2.53(3H×3/4, s), 2.54 (3H×1/4, s), 2.85 (3H×1/4, s), 2.95 (3H×3/4, s), 3.18(1H, dd, J=5, 14 Hz), 3.35 (1H, m), 4.37 (1H×3/4, d, J=15 Hz), 4.54(2H×1/4, s), 4.57 (1H, m), 4.63 (1H×3/4, d, J=15 Hz), 4.82 (1H, m), 6.56(1H, d, J=7 Hz), 7.08-7.20 (3H, m), 7.43 (1H, dd, J=2, 8 Hz), 7.53 (1H,m), 7.58 (1H, m), 8.33 (1H, d, J=2 Hz), 8.49 (1H, d, J=5 Hz)

(6) MASS: 481 (M⁺ +1); NMR (CDCl₃, f): 0.87 (3H, t, J=7 Hz), 1.31 (4H,m), 1.44 (9H, s), 1.61 (1H, m), 1.72 (1H, m), 1.94 (1H, m), 2.05 (1H,m), 2.11 (3H, s), 2.54 (3H, s), 2.56 (2H, m), 2.89 (3H×1/4, s), 3.00(3H×3/4, s), 4.28 (1H, m), 4.44 (1H×3/4, d, J=15 Hz), 4.54 (1H×1/4, d,J=16 Hz), 4.63 (1H×1/4, d, J=16 Hz), 4.65 (1H×3/4, d, J=15 Hz), 4.89(1H, m), 5.22 (1H, m), 6.94 (1H, d, J=7 Hz), 7.13 (1H×3/4, d, J=8 Hz),7.17 (1H×1/4, d, J=8 Hz), 7.46 (1H, dd, J=2, 8 Hz), 8.35 (1H, d, J=2 Hz)

(7) MASS (m/z): 437 (M⁺ +1); NMR (CDCl₃, δ): 0.87 (3H, t, J=7 Hz), 1.33(4H, m), 1.44 (9H, s), 1.67 (2H, m), 2.54 (3H×3/4, s), 2.55 (3H×1/4, s),2.88 (3H×1/4, s), 3.02 (3H×3/4, s), 3.63 (1H, m), 3.96 (1H, m), 4.23(2H, m), 4.47 (1H×1/4, d, J=16 Hz), 4.51 (1H×3/4, d, J=15 Hz), 4.61(1H×3/4, d, J=15 Hz), 4.70 (1H×1/4, d, J=16 Hz), 4.85 (1H, m), 5.56 (1H,d, J=7 Hz), 7.13 (1H, d, J=8 Hz), 7.21 (1H, d, J=7 Hz), 7.46 (1H×3/4, d,J=2, 8 Hz), 7.57 (1H×1/4, d, J=2, 8 Hz), 8.34 (1H×3/4, d, J=2 Hz), 8.48(1H×1/4, d, J=2 Hz)

(8) MASS: 597 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.29 (3H, s),2.33-2.50 (4H, m), 2.53 (3×3/4H, s), 2.58 (1H, dd, J=16 and 2 Hz), 2.78(3×1/4H, s), 2.98-3.09 (2H, m), 3.12-3.28 (1H, m), 3.40-3.50 (2H, m),3.58-3.65 (2H, m), 3.79 (3×1/4H, s), 3.81 (3×3/4H, s), 3.89 (2×1/8H, d,J=16 Hz), 4.28 (2×1/8H, d, J=16 Hz), 4.38 (2×3/8H, d, J=15 Hz), 4.50(2×3/8H, d, J=15Hz), 4.49-4.59 (1H, m), 5.07 (1×3/4H, q, J=8 Hz), 5.19(1×1/4H, q, J=8 Hz), 6.02 (1H, d, J=8 Hz), 6.88 (1×1/4H, s), 7.03(1×3/4H, s), 7.13-7.23 (5H, m), 7.43 (1×1/4H, d, J=8 Hz), 7.47 (1×3/4H,d, J=8 Hz), 7.82 (1×1/4H, s), 7.98 (1×3/4H, s), 8.19 (1×1/4H, d, J=2Hz), 8.21 (1×3/4H, d, J=2 Hz)

(9) NMR (CDCl₃, δ): 1.43 (9H, s), 2.29 (3H, s), 2.31-2.50 (4H, m), 2.60(3×2/3H, s), 2.70 (3×1/3H, s), 2.90-3.30 (4H, m), 3.40-3.53 (2H, m),3.53-3.70 (2H, m), 3.77 (3×1/3H, s), 3.81 (3×2/3H, s), 4.31 (2×1/2H, d,J=15 Hz), 4.43-4.58 (1×2/3H, m), 4.60 (2×1/2H, d, J=15 Hz), 5.08(1×2/3H, q, J=8 Hz), 5.32-5.46 (1×1/3H, m), 5.77 (1×1/3H, q, J=8 Hz),6.02 (1H, t, J=8 Hz), 6.70-6.80 (1H, m), 7.10-7.33 (5H, m), 7.43(1×2/3H, d, J=8 Hz), 7.50 (1×1/3H, d, J=8 Hz), 8.00 (1×1/3H, s), 8.20(1×2/3H, s), 8.38-8.47 (1H, m)

(10) MASS: 645 (M+1); NMR (CDCl₃, δ): 1.47 (9H, s), 2.30 (3H, s),2.32-2.50 (4H, m), 2.50-2.71 (1H, m), 2.56 (3×4/5H, s), 2.78 (3×1/5H,s), 2.96-3.13 (2H, m), 3.14-3.29 (1H, m), 3.42-3.50 (2H, m), 3.58-3.67(2H, m), 4.11 (2×1/10H, d, J=15 Hz), 4.19 (2×2/5H, d, J=16 Hz), 4.22(2×1/10H, d, J=15 Hz), 4.61 (2×2/5H, d, J=16 Hz), 4.48-4.58 (1H, m),5.00-5.13 (1H, m), 5.98-6.08 (1H, m), 7.12-7.23 (5H, m), 7.32 (1×1/5H,s), 7.62 (1×4/5H, s), 7.40 (1×1/5H, d, J=8 Hz), 7.47 (1×4/5H, d, J=8Hz), 8.10 (1×1/5H, s), 8.27 (1×4/5H, s), 8.52 (1×1/5H, s), 8.58 (1×4/5H,s)

Preparation 107

The following object compounds were obtained according to a similarmanner to that of Preparation 3, 4, 8, 41 or 54.

(1) MASS: 497 (M+1); NMR (CDCl₃, δ): 0.88 (3×1/4H, t, J=8 Hz), 0.89(3×3/4H, t, J=8 Hz), 1.20-1.42 (4H, m), 1.58-1.82 (2H, m), 2.60-2.90(2H, m), 2.93 (3×1/4H, s), 3.06 (3×3/4H, s), 3.40-3.50 (2H, m),3.50-3.72 (6H, m), 3.80-3.98 (1H, m), 4.58 (2×1/8H, d, J=16 Hz), 4.59(2×3/8H, d, J=15 Hz), 4.69 (2×3/8H, d, J=15 Hz), 4.71 (2×1/8H, d, J=16Hz), 4.80-5.00 (1H, m), 7.33-7.45 (1H, m), 7.63-7.80 (2H, m), 8.18 (1H,d, J=8 Hz), 8.30 (1H, d, J=8 Hz), 8.53-8.70 (2H, m), 9.18 (1H, s)

(2) MASS: 461 (M+1); NMR (CDCl₃, δ): 0.83 (3×1/4H, t, J=8 Hz), 0.89(3×3/4H, t, J=8 Hz), 1.10-1.40 (4H, m), 1.52-1.80 (2H, m), 2.97 (3×1/4H,s), 3.10 (3×3/4H, s), 3.00-3.13 (1H, m), 3.25-3.38 (1H, m), 3.70-3.79(1×1/4H, m), 3.80-3.85 (1×3/4H, m), 4.57 (2×3/8H, d, J=15 Hz), 4.71(2×3/8H, d, J=15 Hz), 4.73 (2×1/4H, s), 4.87-5.01 (1H, m), 7.18 (1H, t,J=5 Hz), 7.22 (1H, d, J=8 Hz), 7.37-7.45 (1H, m), 7.61 (1H, t, J=8 Hz),7.68-7.81 (2H, m), 8.18 (1×1/4H, d, J=8 Hz), 8.20 (1×3/4H, d, J=8 Hz),8.31 (1H, d, J=8 Hz), 8.52 (1H, d, J=2 Hz), 8.59 (1H, s), 8.63 (1H, d,J=2 Hz), 9.18 (1H, s)

(3) MASS: 444 (M+1); NMR (CDCl₃, δ): 0.85 (3×1/4H, t, J=8 Hz), 0.89(3×3/4H, t, J=8 Hz), 1.20-1.45 (4H, m), 1.57-1.90 (3H, m), 2.09-2.22(1H, m), 2.10 (3H, s), 2.61 (2H, t, J=8 Hz), 2.94 (3×1/4H, s), 3.09(3×3/4H, s), 3.43-3.60 (1H, m), 4.58 (2×3/8H, d, J=15 Hz), 4.71 (2×3/8H,d, J=15 Hz), 4.70 (2×1/8H, d, J=16 Hz), 4.75 (2×1/8H, d, J=16 Hz),4.88-5.12 (1H, m), 7.40 (1H, dd, J=8, 5 Hz), 7.64-7.81 (2H, m), 7.87(1H, d, J=8 Hz), 8.30 (1H, dd, J=8, 2 Hz), 8.59 (1H, s), 8.63 (1H, d,J=2 Hz), 9.18 (1H, s)

(4) NMR (CDCl₃, δ): 0.88 (3H, t, J=7 Hz), 1.33 (4H, m), 1.66 (2H, m),2.55 (3H, s), 2.67 (1H, dd, J=7, 15 Hz), 2.86 (1H, dd, J=3, 15 Hz), 2.91(3H×1/4, s), 3.02 (3H×3/4, s), 3.47 (2H, m), 3.67 (6H, m), 3.73 (1H, m),4.43 (1H×3/4, d, J=15 Hz), 4.63 (2H×1/4, s), 4.68 (1H×3/4, d, J=15 Hz),4.89 (1H, m), 7.13 (1H×3/4, d, J=8 Hz), 7.16 (1H×1/4, d, J=8 Hz), 7.47(1H, m), 8.10 (1H, m), 8.36 (1H, d, J=2 Hz)

(5) NMR (CDCl₃, δ): 0.86 (3H, t, J=7 Hz), 1.22 (4H, m), 1.52-1.73 (2H,m), 2.53 (3H, s), 2.90 (3H×1/4, s), 3.01 (3H×3/4, s), 3.02-3.07 (1H, m),3.26-3.34 (1H, m), 3.73 (1H×1/4, dd, J=3, 7 Hz), 3.80 (1H×3/4, dd, J=3,7 Hz), 4.42 (1H×3/4, d, J=15 Hz), 4.63 (2H×1/4, s), 4.67 (1H×3/4, d,J=15 Hz), 4.90 (1H, m), 7.12-7.37 (3H, m), 7.47 (1H, m), 7.62 (1H, m),8.17 (1H, m), 8.35 (1H, s)

(6) NMR (CDCl₃, δ): 0.89 (3H, t, J=7 Hz), 1.31 (4H, m), 1.70 (2H, m),1.83 (1H, m), 2.11 (3H, s), 2.15 (1H, m), 2.54 (3H, s), 2.62 (2H, t, J=7Hz), 2.92 (3H×1/4, s), 3.03 (3H×3/4, s), 3.47 (1H×1/4, m), 3.53 (1H×3/4,m), 4.43 (1H×3/4, d, J=15 Hz), 4.60 (1H×1/4, d, J=16 Hz), 4.66 (1H×1/4,d, J=16 Hz), 4.67 (1H×3/4, d, J=15 Hz), 4.92 (1H, m), 7.13 (1H×3/4, d,J=8 Hz), 7.17 (1H×1/4, d, J=8 Hz), 7.47 (1H, d, J=8 Hz), 7.84 (1H, d,J=8 Hz), 8.35 (1H, s)

(7) NMR (CDCl₃, δ): 0.88 (3H, t, J=7 Hz), 1.32 (4H, m), 1.73 (2H, m),2.54 (3H, s), 2.91 (3H×1/4, s), 3.02 (3H×3/4, s), 3.47 (1H, m), 3.67(1H, m), 3.82 (1H, m), 4.47 (1H×3/4, d, J=15 Hz), 4.53 (1H×1/4, d, J=16Hz), 4.65 (1H×3/4, d, J=15 Hz), 4.69 (1H×1/4, d, J=16 Hz), 4.88 (1H, m),7.13 (1H×3/4, d, J=8 Hz), 7.19 (1H×1/4, d, J=8 Hz), 7.47 (1H×3/4, m),7.53 (1H×1/4, m), 7.71 (1H, m)

(8) MASS: 497 (M+1); NMR (CDCl₃, δ): 2.31 (3H, s), 2.33-2.45 (4H, m),2.43-2.53 (1H, m), 2.68 (3×3/4H, s), 2.71-2.85 (1H, m), 2.81 (3×1/4H,s), 2.97-3.16 (2H, m), 3.38-3.50 (2H, m), 3.52-3.73 (3H, m), 3.80(3×1/4H, s), 3.83 (3×3/4H, s), 4.10 (2×1/8H, d, J=16 Hz), 4.40 (2×1/8H,d, J=16 Hz), 4.41 (2×3/8H, d, J=15 Hz), 4.54 (2×3/8H, d, J=15 Hz), 5.10(1×3/4H, q, J=8 Hz), 5.19 (1×1/4H, q, J=8 Hz), 6.94 (1×1/4H, s), 7.06(1×3/4H, s), 7.13-7.33 (5H, m), 7.90 (1×1/4H, s), 8.01 (1×3/4H, s), 8.11(1×1/4H, s), 8.17 (1×3/4H, s), 8.20 (1×1/4H, s), 8.22 (1×3/4H, s)

(9) NMR (CDCl₃, δ): 2.31 (3H, s), 2.39-2.60 (4H, m), 2.74 (3×2/3H, s),2.80 (3×1/3H, s), 2.76-2.86 (1H, m), 2.92-3.10 (3H, m), 3.40-3.50 (2H,m), 3.52-3.72 (2H, m), 3.67-3.72 (1×2/3H, m), 3.75-3.81 (1×1/3H, m),3.81 (3×1/3H, s), 3.82 (3×2/3H, s), 3.87 (2×1/6H, d, J=16 Hz), 4.41(2×1/6H, d, J=16 Hz), 4.42 (2×1/3H, d, J=15 Hz), 4.56 (2×1/3H, d, J=15Hz), 5.10 (1×2/3H, q, J=8 Hz), 5.37 (1×1/3H, q, J=8 Hz), 6.73 (1×1/3H,d, J=8 Hz), 6.78 (1×2/3H, d, J=8 Hz), 7.10-7.31 (5H, m), 8.06 (1×1/3H,s), 8.21 (1×2/3H, s), 8.11-8.20 (1H, m), 8.41 (1H, d, J=8 Hz)

(10) MASS: 545 (M+1); NMR (CDCl₃, δ): 2.40 (3H, s), 2.43-2.64 (5H, m),2.68 (3×4/5H, s), 2.71-2.88 (1H, m), 2.81 (3×1/5H, s), 2.97-3.14 (2H,m), 3.47-3.58 (2H, m), 3.60-3.83 (3H, m), 4.18 (2×1/8H, d, J=16 Hz),4.30 (2×3/8H, d, J=15 Hz), 4.38 (2×1/8H, d, J=16 Hz), 4.58 (2×3/8H, d,J=15 Hz), 5.10 (1H, q, J=8 Hz), 7.11-7.30 (5H, m), 7.46 (1×1/4H, s),7.68 (1×3/4H, s), 8.18 (1H, q, J=8 Hz), 8.20 (1×1/4H, s), 8.30 (1×3/4H,s), 8.58 (1×1/4H, s), 8.60 (1×3/4H, s)

Preparation 108

The following compound was obtained according to a similar manner tothat of Preparation 23.

MASS: 201 (M+1); NMR (CDCl₃, δ): 2.49 (3H, s), 3.77 (2H, s), 7.84 (1H,s), 8.47 (1H, s), 8.57 (1H, s)

Preparation 109

To a solution of Starting Compound (1.02 g) in toluene (6 ml) was addedLawesson's reagent (1.29 g), and the mixture was refluxed for 24 hours.After the mixture was allowed to cool to room temperature, it wassubjected to silica gel column chromatography (hexane) to collect ayellow bond. The eluate was evaporated and recrystallized from hexane togive Object Compound (600 mg) as yellow crystals.

mp: 78-79° C.; NMR (CDCl₃, δ): 4.28 (3H, s), 7.22-7.74 (5H, m)

Preparation 110

The following object compound was obtained according to a similar mannerto that of Preparation 1, 6, 11, 38, 52 or 56.

MASS (m/z): 368 (M+H)⁺ ; NMR (CDCl₃, δ): 1.42 (9H, s), 1.72-2.00 (2H,m), 2.02 (1/4×3H, s), 2.08 (3/4×3H, s), 2.52 (3H, s), 2.53 (2H, m), 2.89(1/4×3H, s), 3.02 (3/4×3H, s), 4.51 (1/4×1H, d, J=17 Hz), 4.53 (3/4×2H,ABq, Δ=0.12, J=15 Hz), 4.72 (1/4×1H, d, J=17 Hz), 4.73-4.97 (1H, m),5.25-5.44 (1H, m), 7.10 (3/4×1H, d, J=8 Hz), 7.15 (1/4×1H, d, J=8 Hz),7.46 (1H, dd, J=8, 2 Hz), 8.36 (1H, d, J=2 Hz)

Preparation 111

The following object compound was obtained according to a similar mannerto that of Preparation 3, 4, 8, 41 or 54.

MASS (m/z): 268 (M+H)⁺ ; NMR (CDCl₃, δ): 1.58-1.95 (2H, m), 2.03(1/4×3H, s), 2.08 (3/4×3H, s), 2.50-2.78 (2H, m), 2.53 (3H, s), 2.92(1/4×3H, s), 2.98 (3/4×3H, s), 3.81-3.94 (1H, m), 4.45 (1/4×1H, d, J=17Hz), 4.56 (3/4×2H, ABq, Δ=0.19, J=15 Hz), 4.72 (1/4×1H, d, J=17 Hz),7.11 (3/4×1H, d, J=8 Hz), 7.16 (1/4×1H, d, J=8 Hz), 7.41 (1/4×1H, dd,J=8, 2 Hz), 7.48 (3/4×1H, dd, J=8, 2 Hz), 8.37 (1H, d, J=2 Hz)

Preparation 112

The following compounds were obtained according to a similar manner tothat of Preparation 1, 6, 11, 38, 52 or 56.

(1) MASS (m/z): 516 (M+H)⁺ ; NMR (CDCl₃, δ): 1.44 (9H, s), 1.56-1.97(2H, m), 1.92 (1/4×3H, s), 1.98 (3/4×3H, s), 2.11-2.26 (2H, m), 2.52(3H, s), 2.83 (1/4×3H, s), 2.97 (3/4×3H, s), 3.08-3.46 (2H, m),4.48-4.62 (1H, m), 4.50 (3/4×2H, ABq, Δ=0.25, J=15 Hz), 4.58 (1/4×2H,s), 4.90-5.13 (1H, m), 6.45-6.63 (1H, m), 7.03-7.68 (6H, m), 8.32 (1H,s), 8.51 (1H, s)

(2) MASS (m/z): 455 (M+H)⁺ ; NMR (CDCl₃, δ): 1.44 (9H, s), 1.75-2.15(2H, m), 2.02 (1/4×3H, s), 2.07 (3/4×3H, s), 2.45-2.59 (5H, m), 2.87(1/4×3H, s), 3.03 (3/4×3H, s), 3.50-3.69 (1H, m), 3.78 (1H, br s),3.85-4.10 (1H, m), 4.10-4.30 (1H, m), 4.46 (1/4×1H, d, J=17 Hz), 4.53(3/4×2H, ABq, Δ=0.13, J=15 Hz), 4.78 (1/4×1H, d, J=17 Hz), 4.98-5.22(1H, m), 5.42-5.58 (1H, m), 7.03-7.62 (3H, m), 8.32 (3/4×1H, s), 8.38(1/4×1H, s)

(3) MASS (m/z): 552 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 1.81-2.10(2H, m), 2.02 (3H×1/4, s), 2.08 (3H×3/4, s), 2.46-2.61 (6H, m), 2.89(3H×1/4, s), 3.02 (3H×3/4, s), 3.16-3.28 (1H, m), 3.37-3.49 (2H, m),3.53-3.75 (6H, m), 4.40 (1H×3/4, d, J=15.0 Hz), 4.48-4.60 (1H+1H×1/4,m), 4.68 (1H, d, J=15.0 Hz), 5.01-5.11 (1H×3/4, m), 5.13-5.22 (1H×1/4,m), 6.02 (1H, d, J=8.5 Hz), 7.12 (1H×3/4, d, J=8.5 Hz), 7.17 (1H×1/4, d,J=8.5 Hz), 7.35 (1H×1/4, d, J=8.5 Hz), 7.43 (1H×3/4, d, J=8.5 Hz), 7.46(1H, dd, J=8.5, 1.0 Hz), 8.36 (1H, d, J=1.0 Hz)

(4) MASS (m/z): 499 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47 (9H, s), 1.79-2.14(4H, m), 2.03 (3H×1/4, s), 2.08 (3H×3/4, s), 2.11 (3H, s), 2.45-2.62(7H, s), 2.89 (3H×1/4, s), 3.03 (3H×3/4, s), 4.20-4.33 (1H, m), 4.44(1H×3/4, d, J=15.0 Hz), 4.54 (1H×1/4, d, J=15.0 Hz), 4.64 (1H×3/4, d,J=15.0 Hz), 4.72 (1H×1/4, d, J=15.0 Hz), 5.02-5.25 (2H, m), 6.93(1H×1/4, d, J=8.5 Hz), 6.98 (1H×3/4, d, J=8.5 Hz), 7.13 (1H×3/4, d,J=8.5 Hz), 7.19 (1H×1/4, d, J=8.5 Hz), 7.46 (1H×3/4, dd, J=8.5, 1.5 Hz),7.48 (1H×1/4, dd, J=8.5, 1.5 Hz), 8.37 (1H, d, J=11.5 Hz)

Preparation 113

The following compounds were obtained according to a similar manner tothat of Preparation 3, 4, 8, 41 or 54.

(1) MASS (m/z): 416 (M+H)⁺ ; NMR (CDCl₃, δ): 1.74-2.03 (2H, m), 2.00(1/4×3H, s), 2.06 (3/4×3H, s), 2.30-2.46 (2H, m), 2.54 (3H, s), 2.88(1/4×3H, s), 3.02 (3/4×3H, s), 3.07-3.38 (2H, m), 3.77-3.97 (1H, m),4.53 (3/42H, ABq, Δ=0.18, J=15 Hz), 4.62 (1/4×2H, ABq, Δ=0.13, J=17 Hz),4.98-5.22 (1H, m), 7.07-7.68 (5H, m), 8.17-8.32 (1H, m), 8.36 (1H, s),8.48-8.55 (1H, m)

(2) MASS (m/z): 355 (M+H)⁺ ; NMR (CDCl₃, δ): 1.80-2.10 (2H, m), 2.02(1/4×3H, s), 2.06 (3/4×3H, s), 2.42-2.58 (5H, m), 2.90 (1/4×3H, s), 3.05(3/4×3H, s), 3.38-4.02 (3H, m), 4.46 (1/4×1H, d, J=17 Hz), 4.54 (3/4×2H,ABq, Δ=0.16, J=15 Hz), 4.78 (1/4×1H, d, J=17 Hz), 5.01-5.22 (1H, m),7.08-7.22 (1H, m), 7.42-7.57 (1H, m), 7.76-7.93 (1H, m), 8.37 (1H, s)

(3) MASS (m/z): 452 (M+H)⁺ ; NMR (CDCl₃, δ): 1.85-2.21 (2H, m), 2.02(3H×1/4, s), 2.09 (3H×3/4, s), 2.49-2.61 (5H, m), 2.73-2.82 (2H, m),2.90 (3H×1/4, s), 3.04 (3H×3/4, s), 3.40-3.50 (2H, m), 3.54-3.74 (7H,m), 4.43 (1H×3/4, d, J=15.0 Hz), 4.59 (1H×1/4, d, J=15.0 Hz), 4.65(1H×3/4, d, J=15.0 Hz), 4.71 (1H×1/4, d, J=15.0 Hz), 5.01-5.21 (1H, m),7.11 (1H×3/4, d, J=8.5 Hz), 7.17 (1H×1/4, d, J=8.5 Hz), 7.48 (1H, dd,J=8.5, 1.0 Hz), 8.14 (1H×1/4, d, J=8.5 Hz), 8.20 (1H×3/4, d, J=8.5 Hz),8.37 (1H, d, J=1.0 Hz)

(4) MASS (m/z): 399 (M+H)⁺ ; NMR (CDCl₃, δ): 1.71-2.22 (4H, m), 2.03(3H×1/4, s), 2.09 (3H×3/4, s), 2.10 (3H, s), 2.45-2.67 (4H, m), 2.55(3H, s), 2.90 (3H×1/4, s), 3.06 (3H×3/4, s), 3.44 (1H×1/4, dd, J=8.5,5.5 Hz), 3.52 (1H×3/4, dd, J=8.5, 5.5 Hz), 4.43 (1H×3/4, d, J=14.5 Hz),4.60 (1H×1/4, d, J=16.0 Hz), 4.67 (1H×3/4, d, J=14.5 Hz), 4.73 (1H×1/4,d, J=16.0 Hz), 5.03-5.22 (1H, m), 7.12 (1H×3/4, d, J=8.5 Hz), 7.17(1H×1/4, d, J=8.5 Hz), 7.47 (1H×3/4, dd, J=8.5, 1.0 Hz), 7.50 (1H×1/4,dd, J=8.5, 1.0 Hz), 7.88-7.98 (1H, m), 8.37 (1H, d, J=1.0 Hz)

Preparation 114

The following compound was obtained according to a similar manner tothat of Preparation 23.

(1) MASS: 153 (M+1); NMR (CDCl₃, δ): 2.43 (3H, s), 3.78 (2H, s), 3.96(3H, s), 6.76 (1H, d, J=7 Hz), 8.35 (1H, s), 8.43 (1H, d, J=7 Hz)

(2) MASS: 153 (M+1); NMR (CDCl₃, δ): 2.43 (3H, s), 3.72 (2H, s), 3.81(3H, s), 7.20 (1H, s), 8.12 (1H, s), 8.19 (1H, d, J=2 Hz)

EXAMPLE 1

To an ice-cooled solution of benzo b!furan-2-carboxylic acid (70 mg),Starting Compound (200 mg), and 1-hydroxybenzotriazole (58 mg) inmethylene chloride (20 ml), was added1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (82 mg). Thesolution was stirred at the same temperature for an hour and at roomtemperature overnight. The mixture was concentrated under vacuum and theresidue was diluted in water and extracted with chloroform. The organiclayer was washed with saturated sodium hydrogencarbonate solution, waterand brine, and was dried over magnesium sulfate. After evaporation, thecrude material obtained was purified on a column of silica gel elutingwith chloroform-methanol (30:1) to give Object Compound (260 mg) as anamorphous solid.

MASS (FAB) (m/z): 610 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28 (3H, s), 2.36-2.50(4H, m), 2.58 (3×2/3H, s), 2.62-2.71 (1H, m), 2.80 (3×1/3H, s),2.98-3.11 (2H, m), 3.27-3.38 (1H, m), 3.42-3.56 (2H, m), 3.66-3.70 (2H,m), 4.11-4.38 (2×2/3H, m), 4.65 (2×1/3H, d, J=15 Hz), 5.02-5.17 (2H, m),6.93-7.06 (2H, m), 7.12-7.21 (6H, m), 7.22-7.32 (3H, m), 7.43 (1H, t,J=8 Hz), 7.50 (1H, s), 7.57 (1H, d, J=8 Hz), 7.63-7.72 (2H, m),8.19-8.23 (1H, m)

EXAMPLE 2

The following object compounds were obtained according to a similarmanner to that of Example 1.

(1) MASS (FAB) (m/z): 626 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28 (3H, s),2.34-2.51 (4H, m), 2.56-2.68 (1H, m), 2.62 (3×2/3H, s), 2.80 (3×1/3H,s), 3.00-3.07 (2H, m), 3.31 (1H, t, J=15 Hz), 3.42-3.58 (2H, m),3.62-3.70 (2H, m), 4.12-4.41 (2×2/3H, m), 4.64 (2×1/3H, d, J=15 Hz),4.98-5.14 (2H, m), 6.98-7.08 (2H, m), 7.12-7.21 (6H, m), 7.23-7.31 (3H,m), 7.37-7.46 (2H, m), 7.68-7.75 (1H, m), 7.80-7.88 (2H, m), 8.13 (1H,d, J=8 Hz)

(2) MASS (FAB) (m/z): 613 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52-2.69 (1H, m),2.63 (3×2/3H, s), 2.83 (3×1/3H, s), 3.01-3.09 (2H, m), 3.30 (1H, t, J=15Hz), 3.41-3.53 (2H, m), 3.62-3.79 (6H, m), 4.12-4.43 (2×2/3H, m), 4.63(2×1/3H, d, J=15 Hz), 4.98-5.13 (2H, m), 6.99-7.21 (7H, m), 7.23-7.33(3H, m), 7.36-7.45 (2H, m), 7.67-7.90 (4H, m), 8.12 (1H, t, J=8 Hz)

(3) MASS (FAB) (m/z): 596 (M+H)⁺ ; NMR (CDCl₃, δ): 2.58-2.70 (1H, m),2.59 (3×2/3H, s), 2.82 (3×1/3H, s), 3.04 (2H, t, J=8 Hz), 3.29 (1H, t,J=15 Hz), 3.42-3.58 (2H, m), 3.63-3.77 (6H, m), 4.12-4.40 (2×2/3H, m),4.66 (2×1/3H, d, J=15 Hz), 5.02-5.16 (2H, m), 6.97-7.33 (11H, m),7.42-7.72 (5H, m), 8.11 (1H, d, J=8 Hz)

(4) MASS (FAB) (m/z): 630 (M+H)⁺ ; NMR (CDCl₃, δ): 2.68 (3×2/3H, s),2.72 (1H, dd, J=15, 7 Hz), 2.83 (3×1/3H, s), 2.95-3.08 (2H, m),3.11-3.22 (1H, m), 3.33-3.48 (2H, m), 3.53-3.68 (6H, m), 4.19-4.42(2×2/3H, m), 4.72 (2×1/3H, d, J=15 Hz), 5.13-5.32 (2H, m), 6.88 (1H, d,J=8 Hz), 6.98-7.12 (6H, m), 7.18 (1H, d, J=8 Hz), 7.22-7.29 (4H, m),7.33 (1H, d, J=8 Hz), 7.59 (1H, s), 8.04-8.22 (2H, m)

(5) MASS (FAB) (m/z): 626 (M+H)⁺ ; NMR (CDCl₃, δ): 2.62 (3×2/3H, s),2.72 (1H, dd, J=15, 7 Hz), 2.83 (3×1/3H, s), 2.93-3.08 (2H, m),3.13-3.22 (1H, m), 3.33-3.50 (2H, m), 3.52-3.68 (6H, m), 3.87 (3H, s),4.17-4.40 (2×2/3H, m), 4.71 (2×1/3H, d, J=15 Hz), 5.12-5.30 (2H, m),6.89-7.00 (3H, m), 7.02-7.16 (8H, m), 7.27-7.33 (3H, m), 7.95-8.13 (2H,m)

(6) MASS (FAB) (m/z): 614 (M+H)⁺ ; NMR (CDCl₃, δ): 2.67 (3×2/3H, s),2.72 (1H, dd, J=15, 8 Hz), 2.82 (3×1/3H, s), 2.99-3.03 (2H, m),3.13-3.24 (1H, m), 3.33-3.49 (2H, m), 3.53-3.68 (6H, m), 4.19-4.41(2×2/3H, m), 4.70 (2×1/3H, d, J=15 Hz), 5.13-5.31 (2H, m), 6.91-7.15(9H, m), 7.25-7.29 (4H, m), 7.32-7.38 (1H, m), 8.02-8.17 (2H, m)

(7) MASS (FAB) (m/z): 597 (M⁺ +1); NMR (CDCl₃, δ): 2.42 (1×1/3H, d, J=15Hz), 2.61 (1H, m), 2.88 (3×1/3H, s), 2.97 (3×2/3H, s), 3.05-3.28 (3H,m), 3.41 (2H, m), 3.55-3.64 (6H, m), 4.30 (1×1/3H, d, J=15 Hz), 4.75(1×2/3H, d, J=15 Hz), 4.85 (1×2/3H, d, J=15 Hz), 5.17 (1H, m), 5.39 (1H,m), 6.98-7.17 (5H, m), 7.22-7.33 (3H, m), 7.37-7.66 (3H, m), 8.00-8.48(3H, m)

(8) MASS (FAB) (m/z): 610 (M⁺ +1); NMR (CDCl₃, δ): 2.27 (3H, s),2.24-2.38 (4H, m), 2.55-2.67 (1H, m), 2.85 (3×1/3H, s), 2.96 (3×2/3H,s), 3.07-3.32 (3H, m), 3.45 (2H, m), 3.62 (2H, m), 4.23 (1×2/3H, d, J=15Hz), 4.53 (1×1/3H, d, J=15 Hz), 4.81 (1×2/3H, d, J=15 Hz), 4.88 (1×1/3H,d, J=15 Hz), 5.14 (1H, m)i, 5.38 (1H, q, J=7 Hz), 6.98-7.33 (10H, m),7.38-7.53 (2H, m), 7.63 (1H, m), 8.03-8.16 (2H, m), 8.37 (1H, m)

(9) MASS (FAB) (m/z): 575 (M⁺ +1); NMR (CDCl₃, δ): 1.75 (1H, m), 2.17(3H, s), 2.15-2.32 (3H, m), 2.69 (1H, dd, J=6, 15 Hz), 2.93-3.03 (3H,m), 3.23-3.67 (12H, m), 5.12 (1H, m), 5.17 (1H, m), 7.00 (1H, d, J=2Hz), 7.12-7.22 (6H, m), 7.30 (1H, t, J=8 Hz), 7.44 (1H, d, J=8 Hz), 7.66(1H, d, J=8 Hz), 7.91 (1H, d, J=7 Hz), 8.04 (1H, d, J=8 Hz)

(10) MASS (FAB) (m/z): 577 (M⁺ +1); NMR (CDCl₃, δ): 2.17 (6×1/3H, s),2.21 (6×2/3H, s), 2.30 (1H, m), 2.65-2.75 (1H, m), 2.72 (3×2/3H, s),2.89 (3×1/3H, s), 2.99 (2H, d, J=7 Hz), 3.09 (1H, m), 3.18-3.27 (2H, m),3.44 (2H, m), 3.52 (1H, m), 3.62 (6H, m), 5.05 (1H, m), 5.18 (1H, m),6.98 (1H, s), 7.12-7.17 (6H, m), 7.30 (1H, d, J=8 Hz), 7.45 (1H, d, J=8Hz), 7.65 (1H, d, J=8 Hz), 7.88 (1H, m), 7.95-8.02 (1H, m)

(11) MASS (FAB) (m/z): 582 (M⁺ +1); NMR (CDCl₃, δ): 2.63-2.76 (2H, m),2.90 (1H, dd, J=7, 13 Hz), 3.19 (3H, s), 3.18-3.25 (1H, m), 3.44 (2H,m), 3.65 (6H, m), 4.75 (1H, q, J=7 Hz), 5.12 (1H, m), 6.88-6.95 (5H, m),7.12 (4H, m), 7.28-7.33 (4H, m), 7.44 (1H, d, J=8 Hz), 7.65 (1H, d, J=8Hz), 7.80 (1H, d, J=7 Hz), 7.94 (1H, d, J=8 Hz)

(12) MASS (FAB) (m/z): 618 (M+H)⁺ ; NMR (CDCl₃, δ): 2.60 (3×2/3H, s),2.72-2.88 (1H, m), 2.82 (3×1/3H, s), 2.91-3.20 (3H, m), 4.16-4.40(2×2/3H, m), 4.65 (2×1/3H, d, J=15 Hz), 4.99-5.17 (2H, m), 5.17 (2H, s),6.98-7.15 (7H, m), 7.27-7.37 (10H, m), 7.45 (1H, t, J=8 Hz), 7.51-7.55(2H, m), 7.68-7.78 (2H, m)

(13) mp: 154° C.; MASS (FAB) (m/z): 542 (M⁺ +1); NMR (CDCl₃, δ): 1.24(3H, t, J=7 Hz), 2.77 (1H, dd, J=7, 16 Hz), 3.02-3.17 (3H, m), 4.17 (2H,q, J=7 Hz), 4.82 (1H, q, J=7 Hz), 5.07 (1H, m), 5.14 (1H, d, J=15 Hz),5.20 (1H, d, J=15 Hz), 6.78 (1H, s), 7.05 (5H, s), 7.14-7.21 (2H, m),7.29-7.37 (5H, m), 7.43 (1H, d, J=8 Hz), 7.54 (1H, d, J=8 Hz), 7.67 (1H,d, J=8 Hz), 9.15 (1H, br s)

EXAMPLE 3

Starting Compound (200 mg), 4-cyclohexylpiperazine (64 mg), and1-hydrobenzotriazole (51 mg) were dissolved in a mixed solvent ofmethylene chloride (20 ml) and N,N-dimethylformamide (10 ml). Themixture was ice-cooled and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimidehydrochloride (73 mg) was added thereto. The mixture was stirred at thistemperature for 1 hour and at room temperature for overnight. Themixture was concentrated under vacuum and residue was diluted in waterand extracted with chloroform. The organic layer was washed withsaturated sodium hydrogencarbonate solution and brine. Afterevaporation, the crude material obtained was purified on a column ofsilica gel eluting with chloroform-methanol (60:1) to give ObjectCompound (210 mg) as an amorphous solid.

MASS (FAB) (m/z): 677 (M+H)⁺ ; NMR (CDCl₃, δ): 0.98-1.21 (5H, m),1.53-1.61 (1H, m), 1.70-1.80 (4H, m), 2.40-2.52 (4H, m), 2.50-2.65 (1H,m), 2.56 (3×2/3H, s), 2.62-2.77 (1H, m), 2.80 (3×1/3H, s), 2.94-3.08(2H, m), 3.18-3.28 (1H, m), 3.35-3.47 (2H, m), 3.52-3.65 (2H, m),4.17-4.36 (2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz), 5.11-5.27 (2H, m),6.93-7.15 (9H, m), 7.22-7.29 (4H, m), 7.43 (1H, d, J=8 Hz), 7.66 (1H, d,J=8 Hz), 7.99-8.12 (2H, m)

EXAMPLE 4

The following object compounds were obtained according to a similarmanner to that of Example 3.

(1) MASS (FAB) (m/z): 637 (M+H)⁺ ; NMR (CDCl₃, δ): 0.84 (3H, t, J=8 Hz),1.41-1.52 (2H, m), 2.27 (2H, t, J=8 Hz), 2.32-2.46 (4H, m), 2.58(3×2/3H, s), 2.62-2.72 (1H, m), 2.80 (3×1/3H, s), 2.95-3.08 (2H, m),3.22-3.31 (1H, m), 3.40-3.51 (2H, m), 3.56-3.70 (2H, m), 4.14-4.38(2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz), 5.10-5.21 (2H, m), 6.95-7.18(10H, m), 7.23-7.30 (3H, m), 7.43 (1H, d, J=8 Hz), 7.65 (1H, d, J=8 Hz),7.89-7.97 (1H, m), 8.04-8.11 (1H, m), 9.87 (1H, br s)

(2) MASS (FAB) (m/z): 594 (M+H)⁺ ; NMR (CDCl₃, δ): 1.28-1.53 (6H, m),1.75-1.92 (2H, m), 2.62-2.76 (1H, m), 2.72 (3×2/3H, s), 2.92 (3×1/3H,s), 2.83-3.19 (3H, m), 4.09 (1H, m), 4.22 (2×1/3H, d, J=15 Hz), 4.39(2×1/3H, s), 4.90 (2×1/3H, d, J=15 Hz), 5.23-5.41 (1H, m), 5.60-5.80(1H, m), 6.85-7.11 (7H, m), 7.12-7.16 (3H, m), 7.22-7.30 (4H, m),7.43-7.50 (1H, m), 7.62-7.68 (1H, m), 8.04 (1×1/3H, d, J=8 Hz), 8.22(1×2/3H, d, J=8 Hz), 8.91 (1×1/3H, d, J=8 Hz), 9.00 (1×2/3H, d, J=8 Hz)

(3) MASS (FAB) (m/z): 667 (M+H)⁺ ; NMR (CDCl₃, δ): 1.27 (3H, t, J=8 Hz),2.58-2.71 (1H, m), 2.65 (3×2/3H, s), 2.89 (3×1/3H, s), 2.99-3.04 (2H,m), 3.28 (1H, t, J=15 Hz), 3.40-3.58 (6H, m), 3.60-3.67 (2H, m), 4.15(2H, q, J=8 Hz), 4.28-4.43 (2×2/3H, m), 4.68 (2×1/3H, d, J=15 Hz),5.05-5.18 (2H, m), 6.98-7.20 (9H, m), 7.26-7.33 (4H, m), 7.45 (1H, d,J=8 Hz), 7.67-7.82 (2H, m), 8.03 (1H, d, J=8 Hz), 9.41 (1H, d, J=8 Hz)

(4) mp: 85-90° C.; MASS (FAB) (m/z): 609 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30(3H, s), 2.33-2.52 (4H, m), 2.57-2.69 (1H, m), 2.62 (3×2/3H, s), 2.73(3×1/3H, s), 2.99-3.07 (2H, m), 3.27-3.36 (1H, m), 3.42-3.55 (2H, m),3.58-3.75 (2H, m), 4.14-4.41 (2×2/3H, m), 4.67 (2×1/3H, m), 5.12 (2H, t,J=8 Hz), 6.95-7.21 (9H, m), 7.23-7.35 (4H, m), 7.43 (1H, d, J=8 Hz),7.69 (1H, d, J=8 Hz), 7.78 (1H, t, J=8 Hz), 8.07 (1H, t, J=8 Hz), 9.37(1H, br s)

(5) MASS (FAB) (m/z): 594 (M+H)⁺ ; NMR (CDCl₃, δ): 1.45-1.69 (6H, m),2.60 (3×2/3H, s), 2.57-2.69 (1H, m), 2.82 (3×1/3H, s), 3.00-3.10 (2H,m), 3.25-3.43 (3H, m), 3.45-3.70 (2H, m), 4.15-4.40 (2×2/3H, m), 4.67(2×1/3H, d, J=15 Hz), 5.02-5.18 (2H, m), 6.95-7.08 (3H, m), 7.12-7.19(6H, m), 7.24-7.32 (4H, m), 7.43 (1H, d, J=8 Hz), 7.69 (1H, d, J=8 Hz),7.73-7.82 (1H, m), 8.14 (1H, t, J=8 Hz), 9.41 (1H, br s)

(6) MASS (FAB) (m/z): 580 (M+H)⁺ ; NMR (CDCl₃, δ): 1.80-1.95 (4H, m),2.53-2.68 (1H, m), 2.61 (3×2/3H, s), 2.82 (3×1/3H, s), 2.98-3.07 (2H,m), 3.17 (1H, t, J=15 Hz), 3.29-3.40 (1H, m), 3.42-3.57 (3H, m),4.18-4.39 (2×2/3H, m), 4.68 (2×1/3H, d, J=15 Hz), 5.10-5.17 (2H, m),6.94-7.16 (9H, m), 7.21-7.30 (4H, m), 7.43 (1H, d, J=8 Hz), 7.66 (1H, d,J=8 Hz), 7.98-8.02 (1H, m), 8.40 (1H, t, J=8 Hz), 9.80 (1H, d, J=10 Hz)

(7) MASS (FAB) (m/z): 612 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52-2.62 (4H, m),2.63 (3×2/3H, s), 2.66-2.73 (1H, m), 2.86 (3×1/3H, s), 2.99-3.08 (2H,m), 3.15-3.26 (1H, m), 3.63-3.70 (2H, m), 3.79-3.93 (2H, m), 4.18-4.42(2×2/3H, m), 4.70 (2×1/3H, d, J=15 Hz), 5.12-5.28 (2H, m), 6.97-7.15(9H, m), 7.24-7.30 (4H, m), 7.46 (1H, d, J=8 Hz), 7.67 (1H, d, J=8 Hz),7.98-8.08 (2H, m)

(8) MASS (FAB) (m/z): 566 (M+H)⁺ ; NMR (CDCl₃, δ): 0.38-0.61 (4H, m),2.52-2.69 (2H, m), 2.71 (3×2/3H, s), 2.89-3.09 (2H, m), 2.92 (3×1/3H,s), 3.11-3.22 (1H, m), 4.19-4.51 (2×2/3H, m), 4.97 (2×1/3H, d, J=15 Hz),5.30-5.50 (1H, m), 5.71-5.94 (1H, m), 6.87-7.08 (6H, m), 7.12-7.18 (3H,m), 7.22-7.28 (4H, m), 7.39-7.50 (2H, m), 7.62 (1H, d, J=8 Hz), 8.18(1×1/3H, d, J=8 Hz), 8.35 (1×2/3H, d, J=8 Hz), 9.10 (1×1/3H, d, J=8 Hz),9.21 (1×2/3H, d, J=8 Hz)

(9) MASS (FAB) (m/z): 673 (M+H)⁺ ; NMR (CDCl₃, δ): 2.63 (3×2/3H, s),2.67-2.80 (1H, m), 2.81 (3×1/3H, s), 2.98-3.08 (2H, m), 3.26 (1H, t, J=8Hz), 3.47-3.53 (2H, m), 3.63-3.92 (6H, m), 4.18-4.39 (2×2/3H, m), 4.72(2×1/3H, d, J=15 Hz), 5.12-5.31 (2H, m), 6.49-6.53 (1H, m), 6.97-7.13(9H, m), 7.2-7.30 (4H, m), 7.47 (1H, d, J=8 Hz), 7.67 (1H, d, J=8 Hz),8.00-8.10 (2H, m), 8.30 (2H, d, J=5 Hz)

(10) MASS (FAB) (m/z): 681 (M+H)⁺ ; NMR (CDCl₃, δ): 1.23 (3H, t, J=8Hz), 2.46-2.58 (4H, m), 2.60 (3×2/3H, s), 2.59-2.75 (1H, m), 2.81(3×1/3H, s), 2.99-3.03 (2H, m), 3.17 (2H, s), 3.20-3.28 (1H, m),3.47-3.51 (2H, m), 3.60-3.73 (2H, m), 4.17 (2H, q, J=8 Hz), 4.19-4.39(2×2/3H, m), 4.71 (2×1/3H, d, J=15 Hz), 5.11-5.25 (2H, m), 6.94-7.14(9H, m), 7.21-7.29 (4H, m), 7.43 (1H, d, J=8 Hz), 7.63 (1H, d, J=8 Hz),7.93-8.07 (2H, m)

(11) MASS (FAB) (m/z): 677 (M+H)⁺ ; NMR (CDCl₃, δ): 1.32-1.47 (4H, m),1.50-1.60 (4H, m), 1.78-1.82 (2H, m), 2.42-2.52 (6H, m), 2.55-3.03 (4H,m), 2.62 (3×2/3H, s), 2.81 (3×1/3H, s), 3.18-3.30 (1H, m), 3.80-3.90(1H, m), 4.18-4.37 (2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz), 4.58-4.62(1H, m), 5.11-5.25 (2H, m), 6.93-7.03 (2H, m), 7.08-7.18 (7H, m),7.25-7.30 (4H, m), 7.44 (1H, d, J=8 Hz), 7.65 (1H, d, J=8 Hz), 7.98-8.13(2H, m)

(12) MASS (FAB) (m/z): 580 (M+H)⁺ ; NMR (CDCl₃, δ): 1.47-1.62 (2H, m),1.70-1.88 (2H, m), 2.04-2.15 (1H, m), 2.20-2.30 (1H, m), 2.62-2.73 (1H,m), 2.70 (3×2/3H, s), 2.86-3.17 (3H, m), 2.92 (3×1/3H, s), 4.21-4.46(2×2/3H, m), 4.23-4.32 (1H, m), 4.93 (2×1/3H, d, J=15 Hz), 5.27-5.43(1H, m), 5.67-5.88 (1H, m), 6.90-7.13 (9H, m), 7.22-7.30 (5H, m), 7.48(1H, d, J=8 Hz), 7.64 (1H, d, J=8 Hz), 8.03 (1×1/3H, d, J=8 Hz), 8.21(1×2/3H, d, J=8 Hz), 9.00 (1×1/3H, d, J=8 Hz), 9.10 (1×2/3H, d, J=8 Hz)

(13) MASS (FAB) (m/z): 637 (M+H)⁺ ; NMR (CDCl₃, δ): 1.99 (3×1/3H, s),2.02 (3×2/3H, s), 2.61 (3×2/3H, s), 2.72 (1H, dd, J=15, 5 Hz), 2.84(3×1/3H, d, J=2 Hz), 2.97-3.07 (2H, m), 3.13-3.26 (1H, m), 3.32-3.42(4H, m), 3.50-3.68 (4H, m), 4.15-4.42 (2×2/3H, m), 4.69 (2×1/3H, t, J=15Hz), 5.11-5.32 (2H, m), 6.93-7.14 (9H, m), 7.22-7.31 (4H, m), 7.46 (1H,d, J=8 Hz), 7.65 (1H, d, J=8 Hz), 7.95-8.17 (2H, m)

(14) MASS (FAB) (m/z): 608 (M+H)⁺ ; NMR (CDCl₃, δ): 0.80-1.11 (3H, m),1.17-1.31 (2H, m), 1.47-1.67 (3H, m), 1.78-1.91 (2H, m), 2.58-2.68 (1H,m), 2.69 (3×2/3H, s), 2.77-2.86 (1H, m), 2.89 (3×1/3H, s), 3.00-3.12(2H, m), 3.61-3.75 (1H, m), 4.20-4.42 (2×2/3H, m), 4.88 (2×1/3H, d, J=15Hz), 5.18-5.31 (1H, m), 5.38-5.52 (1H, m), 6.38 (1H, t, J=8 Hz),6.98-7.10 (9H, m), 7.21-7.32 (4H, m), 7.45 (1H, dd, J=8, 2 Hz) 7.63 (1H,dd, J=8, 2 Hz), 7.96 (1×1/3H, d, J=8 Hz), 8.07 (1×2/3H, d, J=8 Hz),8.60-8.67 (1H, m)

(15) MASS (FAB) (m/z): 610 (M+H)⁺ ; NMR (CDCl₃, δ): 2.21 (6×1/3H, s),2.23 (6×2/3H, s), 2.41-2.57 (3H, m), 2.59 (3×2/3H, s), 2.64-2.73 (1H,m), 2.81 (3×1/3H, s), 2.97-3.03 (2H, m), 3.02 (3H, s), 3.18-3.60 (2H,m), 4.17-4.38 (2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz), 5.10-5.21 (2H, m),6.94-7.06 (2H, m), 7.10-7.18 (7H, m), 7.23-7.31 (4H, m), 7.45 (1H, d,J=8 Hz), 7.65 (1H, d, J=8 Hz), 7.89-8.00 (1H, m), 8.11-8.23 (1H, m),9.90 (1H, br s)

(16) MASS (FAB) (m/z): 623 (M+H)⁺ ; NMR (CDCl₃, δ): 1.82-1.97 (2H, m),2.32 (3H, s), 2.51-2.73 (5H, m), 2.62 (3×2/3H, s), 2.81 (3×1/3H, s),2.94-3.08 (2H, m), 3.20-3.30 (1H, m), 3.42-3.75 (4H, m), 4.14-4.39(2×2/3H, m), 4.68 (2×1/3H, dd, J=15, 5 Hz), 5.09-5.21 (2H, m), 6.97-7.05(2H, m), 7.10-7.15 (6H, m), 7.22-7.30 (5H, m), 7.45 (1H, d, J=8 Hz),7.66 (1H, d, J=8 Hz), 7.91-8.00 (1H, m), 8.14-8.23 (1H, m)

(17) MASS (FAB) (m/z): 597; NMR (CDCl₃, δ): 2.13 (6H, s), 2.41 (2H, t,J=5 Hz), 2.70 (3×2/3H, s), 2.62-2.80 (1H, m), 2.90 (3×1/3H, s),2.98-3.10 (3H, m), 3.27-3.35 (2H, m), 4.28-4.43 (2×2/3H, m), 4.83(2×1/3H, d, J=15 Hz), 5.18-5.30 (1H, m), 5.35-5.49 (1H, m), 6.98-7.13(9H, m), 7.22-7.31 (5H, m), 7.45 (1H, d, J=8 Hz), 7.65 (1H, d, J=8 Hz),7.92-8.05 (1H, m), 8.62 (1H, d, J=8 Hz)

(18) MASS (FAB) (m/z): 615; NMR (CDCl₃, δ): 2.52-2.70 (1H, m), 2.73(3×2/3H, s), 2.92 (3×1/3H, s), 2.75-2.90 (1H, m), 2.97-3.12 (2H, m),4.12 (1H, d, J=15 Hz), 4.33 (1H, d, J=15 Hz), 4.22-4.39 (2×2/3H, m),4.83 (2×1/3H, d, J=15 Hz), 5.22-5.34 (1H, m), 5.50-5.62 (1H, m),6.86-7.14 (14H, m), 7.21-7.31 (5H, m), 7.48 (1H, d, J=8 Hz), 7.66 (1H,d, J=8 Hz), 7.86 (1×1/3H, d, J=8 Hz), 7.97 (1×2/3H, d, J=8 Hz) 8.75 (1H,d, J=8 Hz)

(19) MASS (FAB) (m/z): 611; NMR (DMSO-d₆, δ): 2.35-2.52 (1H, m),2.68-2.73 (4H, m), 2.81 (3×1/2H, s), 2.83 (3×1/2H, s), 2.76-3.03 (4H,m), 3.40-3.80 (3H, m), 4.34-4.56 (2H, m), 4.80-5.02 (2H, m), 7.02-7.33(13H, m), 7.45 (1H, d, J=8 Hz), 7.65 (1H, d, J=8 Hz), 8.12-8.40 (1H, m),8.43-8.62 (1H, m), 8.87 (1H, m)

(20) MASS (FAB) (m/z): 540; NMR (CDCl₃, δ): 2.65-2.69 (4H, m), 2.73(3×2/3H, s), 2.97 (3×1/3H, s), 2.87-3.15 (3H, m), 4.29-4.49 (2×2/3H, m),4.82 (2×1/3H, d, J=15 Hz), 5.23-5.42 (1H, m), 5.61-5.78 (1H, m),6.85-6,93 (2H, m), 7.02-7.14 (8H, m), 7.16 (1H, d, J=8 Hz), 7.18-7.30(3H, m), 7.48 (1H, d, J=8 Hz), 7.65 (1H, d, J=8 Hz), 8.05 (1×1/3H, d,J=8 Hz), 8.17 (1×2/3H, d, J=8 Hz), 8.93 (1H, t, J=8 Hz) (21) NMR (CDCl₃,δ): 2.20-2.30 (1×1/2H, m), 2.52-2.62 (1×1/2H, m), 2.83 (3×2/3H, m),2.94-2.99 (1H, m), 3.00 (3×1/3H, s), 3.42-3.95 (3H, m), 4.18-4.70 (2H,m), 5.26 (1H, t, J=8 Hz), 6.83-6.88 (2H, m), 7.02-7.38 (15H, m), 7.52(1×1/2H, d, J=8 Hz), 7.60 (1×1/2H, d, J=8 Hz), 7.80 (1×1/2H, d, J=8 Hz),8.00 (1×1/2H, s), 9.04 (1×1/2H, s), 9.22 (1×1/2H, s)

(22) MASS (FAB) (m/z): 672 (M+H)⁺ ; NMR (CDCl₃, δ): 2.61 (3×2/3H, s),2.67-2.80 (1H, m), 2.80 (3×1/3H, s), 2.97-3.04 (2H, m), 3.22-3.31 (1H,m), 3.42-3.62 (6H, m), 3.70-3.81 (2H, m), 4.17-4.38 (2×2/3H, m), 4.71(2×1/3H, d, J=15 Hz), 5.12-5.22 (1H, m), 5.25-5.30 (1H, m), 6.57 (1H, d,J=8 Hz), 6.65 (1H, t, J=8 Hz), 6.95-7.05 (4H, m), 7.10-7.14 (6H, m),7.23-7.28 (3H, m), 7.42-7.49 (2H, m), 7.67 (1H, d, J=8 Hz), 8.01-8.10(2H, m), 8.18 (1H, d, J=5 Hz)

(23) MASS (FAB) (m/z): 639 (M+H)⁺ ; NMR (CDCl₃, δ): 2.38-2.51 (6H, m),2.61 (3×2/3H, s), 2.63-2.73 (1H, m), 2.82 (3×1/3H, s), 2.98-3.06 (2H,m), 3.18-3.28 (1H, m), 3.40-3.48 (2H, m), 3.60-3.70 (4H, m), 4.16-4.39(2×2/3H, m), 4.70 (2×1/3H, d, J=15 Hz), 5.11-5.23 (2H, m), 6.96-7.13(9H, m), 7.22-7.28 (4H, m), 7.43 (1H, d, J=8 Hz), 7.65 (1H, d, J=8 Hz),7.97-8.09 (2H, m)

(24) MASS (FAB) (m/z): 554 (M+H)⁺ ; NMR (CDCl₃, δ): 2.60 (3×2/3H, s),2.56-2.70 (1H, m), 2.82 (3×1/3H, s), 2.95 (6H, s), 3.00-3.06 (2H, m),3.24 (1H, t, J=15 Hz), 4.19-4.39 (2×2/3H, m), 4.68 (2×1/3H, d, J=15 Hz),5.09-5.20 (2H, m), 6.93-7.05 (3H, m), 7.08-7.16 (6H, m), 7.23-7.30 (4H,m), 7.43 (1H, d, J=8 Hz), 7.63 (1H, d, J=8 Hz), 7.99 (1H, t, J=8 Hz),8.17-8.25 (1H, m)

(25) MASS (FAB) (m/z): 671 (M+H)⁺ ; NMR (CDCl₃, δ): 2.62 (3×2/3H, s),2.65-2.81 (1H, m), 2.82 (3×1/3H, s), 3.02 (2H, t, J=8 Hz), 3.08-3.20(4H, m), 3.22-3.38 (1H, m), 3.50-3.65 (2H, m), 3.70-3.82 (2H, m),4.16-4.39 (2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz), 5.11-5.20 (1H, m),5.21-5.28 (1H, m), 6.89 (3H, t, J=8 Hz), 6.95-7.13 (9H, m), 7.22-7.31(6H, m), 7.45 (1H, d, J=8 Hz), 7.66 (1H, d, J=8 Hz), 7.98-8.11 (2H, m)

(26) MASS (FAB) (m/z): 596 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.67 (1H, m),2.61 (3×2/3H, s), 2.79 (3×1/3H, s), 2.92-3.09 (2H, m), 3.21-3.48 (3H,m), 3.62-3.68 (6H, m), 4.15-4.42 (2×2/3H, m), 4.65 (2×1/3H, d, J=15 Hz),5.11-5.23 (2H, m), 6.96-7.37 (13H, m), 7.75-7.93 (3H, m), 8.07 (1H, d,J=8 Hz)

(27) MASS (FAB) (m/z): 624 (M+H)⁺ ; NMR (CDCl₃, δ): 1.87-2.03 (2H, m),2.35 (3H, s), 2.57-2.72 (5H, m), 2.60 (3×2/3H, s), 2.80 (3×1/3H, s),3.00-3.12 (2H, m), 3.32 (1H, t, J=15 Hz), 3.47-3.76 (4H, m), 4.10-4.37(2×2/3H, m), 4.65 (2×1/3H, dd, J=15, 8 Hz), 5.02-5.18 (2H, m), 6.92-7.08(2H, m), 7.13-7.21 (5H, m), 7.23-7.32 (4H, m), 7.45 (1H, t, J=8 Hz),7.52 (1H, s), 7.58 (1H, d, J=8 Hz), 7.69 (1H, d, J=8 Hz), 7.72-7.83 (1H,m), 8.27-8.33 (1H, m)

(28) MASS (FAB) (m/z): 678 (M+H)⁺ ; NMR (CDCl₃, δ): 1.00-1.30 (5H, m),1.58-1.68 (2H, m), 1.72-1.87 (4H, m), 2.50-2.61 (4H, m), 2.58 (3×2/3H,s), 2.67 (1H, dd, J=15, 7 Hz), 2.80 (3×1/3H, s), 2.99-3.11 (2H, m), 3.32(1H, t, J=8 Hz), 3.40-3.55 (2H, m), 3.61-3.70 (2H, m), 4.12-4.38(2×2/3H, m), 4.67 (2×1/3H, d, J=8 Hz), 5.02-5.18 (2H, m), 6.95-7.08 (2H,m), 7.13-7.20 (5H, m), 7.25-7.33 (4H, m), 7.45 (1H, s), 7.51 (1H, s),7.58 (1H, d, J=8 Hz), 7.64-7.73 (2H, m), 8.22-8.28 (1H, m)

(29) MASS (FAB) (m/z): 638 (M+H)⁺ ; NMR (CDCl₃, δ): 0.90 (3H, t, J=8Hz), 1.51 (2H, q, J=8 Hz), 2.32 (2H, t, J=8 Hz), 2.38-2.52 (4H, m), 2.62(3×2/3H, s), 2.68 (1H, dd, J=15, 7 Hz), 2.83 (3×1/3H, s), 3.02-3.12 (2H,m), 3.31 (1H, t, J=8 Hz), 3.43-3.58 (2H, m), 3.65-3.71 (2H, m),4.12-4.40 (2×2/3H, m), 4.67 (2×1/3H, d, J=15 Hz), 5.02-5.18 (2H, m),6.93-7.08 (2H, m), 7.14-7.20 (5H, m), 7.23-7.32 (4H, m), 7.43 (1H, t,J=8 Hz), 7.50 (1H, s), 7.58 (1H, d, J=8 Hz), 7.63-7.73 (2H, m),8.20-8.26 (1H, m)

(30) MASS (FAB) (m/z): 674 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53 (3×2/3H, s),2.72 (1H, dd, J=15, 7 Hz), 2.79 (3×1/3H, s), 2.97-3.12 (2H, m), 3.36(1H, t, J=15 Hz), 3.48-3.62 (2H, m), 3.68-3.75 (2H, m), 3.79-3.99 (4H,m), 4.11-4.40 (2×2/3H, m), 4.63 (2×1/3H, d, J=15 Hz), 5.07-5.19 (2H, m),6.53 (1H, t, J=5 Hz), 6.97-7.08 (2H, m), 7.12-7.20 (5H, m), 7.23-7.31(4H, m), 7.42 (1H, t, J=8 Hz), 7.48 (1H, s), 7.57 (1H, d, J=8 Hz),7.62-7.73 (2H, m), 8.23 (1H, d, J=8 Hz), 8.32 (2H, d, J=8 Hz)

(31) MASS (FAB) (m/z): 521 (M⁺ 1); NMR (CDCl₃, δ): 1.21 (3H, t, J=7 Hz),2.57 (1H, dd, J=7, 16 Hz), 3.08 (2H, m), 3.23 (1H, dd, J=4, 16 Hz),3.38-3.52 (2H, m), 3.62-3.70 (6H, m), 4.13 (2H, q, J=7 Hz), 4.77 (1H, q,J=7 Hz), 5.08 (1H, m), 6.92 (1H, d, J=2 Hz), 7.13 (5H, s), 7.31 (1H, t,J=8 Hz), 7.43 (1H, d, J=8 Hz), 7.54 (1H, d, J=8 Hz), 7.67 (1H, d, J=8Hz), 8.07 (1H, d, J=7 Hz), 9.38 (1H, br s)

EXAMPLE 5

The following object compound was obtained according to a similar mannerto that of Preparation 13.

MASS: (FAB) (m/z): 493 (M⁺ +1); NMR (DMSO-d₆, δ): 2.78 (2H, m), 2.94(1H, m), 3.04 (1H, m), 3.37-3.58 (8H, m), 4.47 (1H, m), 4.94 (1H, q, J=7Hz), 7.02-7.09 (3H, m), 7.14-7.22 (5H, m), 7.45 (1H, d, J=8 Hz), 7.64(1H, d, J=8 Hz), 7.95 (1H, d, J=8 Hz), 8.58 (1H, d, J=7 Hz)

EXAMPLE 6

The following object compound was obtained according to a similar mannerto that of Preparation 10.

mp: 245-250° C.; NMR (DMSO-d₆, δ): 2.42-2.60 (1H, m), 2.71 (3×1/3H, s),2.77 (3×2/3H, s), 2.81-2.93 (1H, m), 2.95-3.03 (1H, m), 3.40-3.48 (1H,m), 4.32 (2×1/3H, d, J=15 Hz), 4.43-4.57 (2×2/3H, m), 4.68-4.77 (1H, m),4.84-5.00 (1H, m), 6.98-7.36 (11H, m), 7.47 (1H, t, J=8 Hz), 7.54 (1H,s), 7.68 (1H, d, J=8 Hz), 7.78 (1H, d, J=8 Hz), 8.71-8.98 (2H, m)

EXAMPLE 7

The following object compound was obtained according to a similar mannerto that of Preparation 10.

MASS (m/z): 452 (M⁺ +1); NMR (CDCl₃, δ): 1.13 (3H, t, J=7 Hz), 2.82 (2H,m), 3.02 (2H, m), 4.07 (2H, q, J=7 Hz), 4.84 (1H, q, J=7 Hz), 5.25 (1H,m), 6.88-7.10 (7H, m), 7.22 (1H, d, J=8 Hz), 7.34 (1H, d, J=8 Hz), 7.55(1H, d, J=8 Hz), 7.69 (1H, br s), 7.87 (1H, br s)

EXAMPLE 8

Starting Compound (496 mg) was dissolved in dichloromethane (1 ml) andcooled to 0° C. Trifluoroacetic acid (1 ml) was added to the solutionand the mixture was stirred at 0° C. for 3 hours. The reaction mixturewas made basic with ice cooling by adding aqueous sodium hydroxide, andextracted three times with chloroform. The organic layer was washed withbrine and dried over magnesium sulfate. Evaporation of the solvent gaveCompound A as white solid. 1H-Indole-2-carboxylic acid (75 mg) wasdissolved in tetrahydrofuran (2 ml) and cooled to -15° C.N-Methyl-morpholine (0.05 ml) and isobutyl chloroformate (73 mg) wereadded to the solution and stirred for 5 minutes. Compound A obtainedabove was dissolved in tetrahydrofuran (2.5 ml), added to the solutionat -15° C., and stirred at 0° C. for 30 minutes. The reaction mixturewas diluted with chloroform, washed with aqueous sodium hydrogencarbonate, washed with brine, and dried over magnesium sulfate.Evaporation of the solvent followed by column chromatography (silicagel, chloroform-methanol) afforded Object Compound (66 mg) as whitepowder.

MASS (m/z): 740 (M+H)⁺ ; NMR (CDCl₃, δ): 2.36 (3H, s), 2.55-2.72 (1H,m), 2.80 (1/3×3H, s), 2.82-3.05 (2H, m), 2.90 (2/3×3H, s), 3.20-3.35(1H, m), 3.35-3.73 (8H, m), 4.20 (2/3×1H, d, J=15 Hz), 4.53 (1/3×2H,ABq, Δ=0.12, J=17 Hz), 4.63 (2/3×1H, d, J=17 Hz), 5.00-5.22 (2H, m),7.00-8.10 (18H, m), 9.65 (1/3×1H, s), 9.68 (2/3×1H, s)

EXAMPLE 9

The following object compounds were obtained according to a similarmanner to that of Example 8.

(1) MASS (m/z): 582 (M+H)⁺ ; NMR (CDCl₃, δ): 2.67-2.75 (1H, m),3.02-3.15 (2H, m), 3.20-3.30 (1H, m), 3.30-3.50 (4H, m), 3.50-3.65 (4H,m), 4.29-4.51 (2H, m), 4.65-4.75 (1H, m), 4.85-4.92 (1H, m), 6.80-7.43(16H, m), 7.63-7.75 (2H, m), 8.97 (1H, br s)

(2) MASS (m/z): 492 (M+H)⁺ ; NMR (DMSO-d₆, δ): 2.67-2.92 (3H, m),3.00-3.09 (1H, m), 3.38-3.60 (8H, m), 4.32-4.41 (1H, m), 4.82-4.92 (1H,m), 6.98-7.24 (10H, m), 7.38 (1H, br s), 7.47 (1H, d, J=8 Hz), 7.65 (1H,d, J=8 Hz), 8.00 (1H, d, J=8 Hz), 8.58 (1H, d, J=8 Hz)

(3) MASS (m/z): 506 (M+H)⁺ ; NMR (CDCl₃, δ): 2.60-2.72 (1H, m), 2.80(2/3×3H, s), 2.92 (1/3×3H, s), 3.28-3.78 (10H, m), 4.03-4.15 (2H, m),4.40 (1/3×2H, s), 4.53 (2/3×2H, ABq, Δ=0.05, J=15 Hz), 5.10-5.23 (1H,m), 7.00-8.23 (11H, m), 9.18 (1/3×1H, br s), 9.22 (2/3×1H, br s)

(4) MASS (m/z): 626 (M+H)⁺ ; NMR (CDCl₃, δ): 2.62 (2/3×3H, s), 2.6-2.7(1H, m), 2.79 (1/3×3H, s), 3.0-3.1 (2H, m), 3.2-3.3 (1H, m), 3.4-3.7(8H, m), 3.78 (3H, s), 4.03 (1/3×1H, d, J=17 Hz), 4.23 (2/3×1H, d, J=15Hz), 4.34 (1/3×1H, d, J=17 Hz), 4.58 (2/3×1H, d, J=15 Hz), 5.1-5.2 (2H,m), 6.8-7.0 (4H, m), 7.1-7.2 (7H, m), 7.3-7.4 (1H, m), 7.44 (1H, d, J=9Hz), 7.68 (1H, d, J=9 Hz), 7.72 (1/3×1H, d, J=9 Hz), 7.76 (2/3×1H, d,J=9 Hz), 8.05 (1H, d, J=9 Hz), 9.35 (1/3×1H, br s), 9.39 (2/3×1H, br s)

(5) MASS (m/z): 582 (M+H)⁺ ; NMR (CDCl₃, δ): 2.63 (1H, dd, J=15, 7 Hz),2.76 (2/3×3H, s), 2.82 (1/3×3H, s), 3.23 (1H, dd, J=15, 3 Hz), 3.4-3.7(8H, m), 4.28 (1/3×1H, d, J=16 Hz), 4.42 (2/3×1H, d, J=14 Hz), 4.55(1/3×1H, d, J=16 Hz), 4.70 (2/3×1H, d, J=14 Hz), 5.1-5.2 (1H, m), 5.78(2/3×1H, d, J=7 Hz), 5.80 (1/3×1H, d, J=7 Hz), 6.9-7.4 (14H, m), 7.62(1H, d, J=7 Hz), 8.07 (1H, d, J=7 Hz), 8.35 (1H, d, J=7 Hz), 9.33 (1H,br s)

(6) MASS (m/z): 702 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52-2.78 (1H, m), 2.67(2/3×3H, s), 2.85 (1/3×3H, s), 2.88-3.05 (2H, m), 3.12-3.30 (1H, m),3.32-3.75 (8H, m), 4.28 (2/3×1H, d, J=15 Hz), 4.33 (1/3×2H, ABq, Δ=0.16,J=17 Hz), 4.68 (2/3×1H, d, J=15 Hz), 4.82 (2H, s), 5.02-5.28 (2H, m),6.62-8.15 (21H, m), 9.83 (1/3×1H, s), 9.87 (2/3×1H, s)

(7) MASS (m/z): 715 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28 (3H, s), 2.28-2.52(4H, m), 2.52-2.71 (1H, m), 2.64 (2/3×3H, s), 2.82 (1/3×3H, s),2.88-3.00 (2H, m), 3.20-3.38 (1H, m), 3.38-3.75 (4H, m), 4.28 (2/3×1H,d, J=15 Hz), 4.32 (1/3×2H, ABq, Δ=0.16, J=17 Hz), 4.67 (2/3×1H, d, J=15Hz), 4.85 (2H, s), 4.98-5.18 (2H, m), 6.65-8.15 (21H, m), 9.42 (1/3×1H,s), 9.46 (2/3×1H, s)

(8) MASS (m/z): 612 (M+H)⁺ ; NMR (CDCl₃, δ): 2.59-2.78 (1H, m), 2.74(2/3×3H, s), 2.80-2.98 (2H, m), 2.83 (1/3×3H, s), 3.10-3.25 (1H, m),3.30-3.70 (8H, m), 4.32 (2/3×1H, d, J=15 Hz), 4.41 (1/3×2H, ABq, Δ=0.14,J=17 Hz), 4.67 (2/3×1H, d, J=15 Hz), 5.02-5.25 (2H, m), 6.47-8.13 (17H,m), 9.95 (1H, s)

(9) MASS (m/z): 610 (M+H)⁺ ; NMR (CDCl₃, δ): 2.45-2.85 (4H, m), 2.64(3/5×3H, s), 2.84 (2/5×3H, s), 2.90-3.02 (2H, m), 3.18-3.40 (2H, m),3.40-3.78 (8H, m), 4.91-5.19 (2H, m), 6.93-8.10 (17H, m), 9.50 (2/5×1H,s), 9.52 (3/5×1H, s)

(10) MASS (m/z): 654 (M+H)⁺ ; NMR (CDCl₃, δ): 2.5-2.7 (1H, m), 2.65(2/3×3H, s), 2.80 (1/3×3H, s), 3.0-3.1 (2H, m), 3.2-3.3 (1H, m), 3.4-3.7(8H, m), 3.92 (3H, s), 4.35 (2/3×1H, d, J=15 Hz), 4.43 (1/3×1H, d, J=15Hz), 4.65 (1/3×1H, d, J=15 Hz), 4.68 (2/3×1H, d, J=15 Hz), 4.8-5.2 (2H,m), 6.9-7.5 (11H, m), 7.6-8.1 (5H, m), 9.19 (1/3×1H, br s), 9.37(2/3×1H, br s)

(11) MASS (m/z): 646 (M+H)⁺ ; NMR (CDCl₃, δ): 2.5-2.7 (1H, m), 2.68(2/3×3H, s), 2.88 (1/3×3H, s), 3.0-3.1 (2H, m), 3.1-3.3 (1H, m), 3.3-3.7(8H, m), 4.30 (1/3×1H, d, J=17 Hz), 4.48 (2/3×1H, d, J=15 Hz), 4.56(1/3×1H, d, J=17 Hz), 4.80 (2/3×1H, d, J=15 Hz), 5.0-5.2 (2H, m),6.9-7.9 (18H, m), 8.08 (1H, d, J=9 Hz), 9.47 (1/3×1H, br s), 9.50(2/3×1H, br s)

(12) MASS (m/z): 646 (M+H)⁺ ; NMR (CDCl₃, δ): 2.40-2.65 (1H, m), 2.60(2/3×3H, s), 2.94 (1/3×3H, s), 2.95-3.10 (2H, m), 3.20-3.80 (9H, m),4.74 (1/3×2H, ABq, Δ=0.10, J=17 Hz), 4.77 (2/3×1H, d, J=15 Hz),4.88-5.20 (2H, m), 5.22 (2/3×1H, d, J=15 Hz), 6.93-8.15 (19H, m), 9.28(1/3×1H, s), 9.35 (2/3×1H, s)

(13) MASS (m/z): 612 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.68 (1H, m), 2.59(2/3×3H, s), 2.72 (1/3×3H, s), 2.95-3.08 (2H, m ), 3.15-3.70 (9H, m),3.75 (1/3×1H, d, J=17 Hz), 4.30 (1/3×1H, d, J=17 Hz), 4.35 (2/3×2H, ABq,Δ=0.06, J=15 Hz), 4.83-5.20 (2H, m), 6.65-8.35 (17H, m), 9.72 (1H, s)

(14) MASS (m/z): 613 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.75 (1H, m), 2.59(2/3×3H, s), 2.75 (1/3×3H, s), 2.95-3.15 (2H, m), 3.20-3.75 (9H, m),3.84 (1/3×1H, d, J=17 Hz), 4.30 (1/3×1H, d, J=17 Hz), 4.38 (2/3×2H, ABq,Δ=0.13, J=15 Hz), 4.82-5.23 (2H, m), 6.68-8.30 (17H, m)

(15) MASS (m/z): 638 (M⁺); NMR (CDCl₃, δ): 2.60 (2/3×3H, s), 2.6-2.7(1H, m), 2.80 (1/3×3H, s), 2.92 (6H, s), 3.0-3.1 (2H, m), 3.2-3.3 (1H,m), 3.4-3.7 (8H, m), 3.98 (1/3×1H, d, J=17 Hz), 4.22 (2/3×1H, d, J=15Hz), 4.34 (1/3×1H, d, J=17 Hz), 4.58 (2/3×1H, d, J=15 Hz), 5.0-5.2 (1H,m), 6.63 (2H, d, J=8 Hz), 6.91 (1/3×2H, d, J=8 Hz), 7.00 (2/3×2H, d, J=8Hz), 7.1-7.2 (7H, m), 7.2-7.3 (1H, m), 7.43 (1H, d, J=7 Hz), 7.67 (1H,d, J=7 Hz), 7.80 (1/3×1H, d, J=8 Hz), 7.85 (2/3×1H, d, J=8 Hz), 8.05(1H, d, J=8 Hz), 9.50 (1/3×1H, br s), 9.57 (2/3×1H, br s)

(16) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.72 (1H, m), 2.80(2/3×3H, s), 2.90 (1/3×3H, s), 2.95-3.32 (3H, m), 3.37-3.74 (8H, m),4.43 (1/3×2H, ABq, Δ=0.05, J=17 Hz), 4.48 (2/3×1H, d, J=15 Hz), 4.70(2/3×1H, d, J=15 Hz), 5.07-5.21 (2H, m), 6.93-8.10 (15H, m), 8.45-8.55(1H, m), 9.63 (1/3×1H, s), 9.65 (2/3×1H, s)

(17) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.72 (1H, m), 2.70(3/4×3H, s), 2.82 (1/4×3H, s), 2.90-3.15 (2H, m), 3.18-3.34 (1H, m),3.38-3.78 (8H, m), 4.28 (1/4×2H, ABq, Δ=0.05, J=17 Hz), 4.31 (3/4×1H, d,J=15 Hz), 4.58 (3/4×1H, d, J=15 Hz), 4.93-5.22 (2H, m), 6.75-8.10 (14H,m), 8.43-8.51 (2H, m), 9.58 (1H, s)

(18) MASS (FAB) (m/z): 668 (M+H)⁺ ; NMR (CDCl₃, δ): 2.23 (3H, s),2.30-2.46 (4H, m), 2.58-2.69 (1H, m), 2.58 (3×2/3H, s), 2.73 (3×1/3H,s), 2.92-3.10 (2H, m), 3.23-3.33 (1H, m), 3.38-3.52 (2H, m), 3.60-3.67(2H, m), 3.88 (3H, s), 4.20-4.35 (2×2/3H, m), 4.66 (2×1/3H, d, J=15 Hz),5.01-5.18 (2H, m), 6.95 (2×1/3H, d, J=8 Hz), 7.03 (2×2/3H, d, J=8 Hz),7.10-7.20 (5H, m), 7.26 (1H, t, J=8 Hz), 7.38 (1H, t, J=8 Hz), 7.47 (1H,s), 7.52 (1H, d, J=8 Hz), 7.65 (1H, d, J=8 Hz), 7.73 (1H, d, J=8 Hz),7.90 (2H, d, J=8 Hz), 8.19 (1H, t, J=8 Hz)

(19) MASS (FAB) (m/z): 655 (M+H)⁺ ; NMR (CDCl₃, δ): 2.58-2.70 (1H, m),2.67 (3×2/3H, s), 2.80 (3×1/3H, s), 2.98-3.13 (2H, m), 3.31 (1H, t, J=15Hz), 3.40-3.57 (2H, m), 3.63-3.77 (6H, m), 3.91 (3H, s), 4.20-4.40(2×2/3H, m), 4.70 (2×1/3H, d, J=15 Hz), 5.03-5.18 (2H, m), 6.99 (2×1/3H,d, J=8 Hz), 7.09 (2×2/3H, d, J=8 Hz), 7.13-7.23 (6H, m), 7.31 (1H, t,J=8 Hz), 7.44 (1H, t, J=8 Hz), 7.51 (1H, s), 7.61 (1H, t, J=8 Hz), 7.70(1H, d, J=8 Hz), 7.93 (2H, d, J=8 Hz), 8.20 (1H, t, J=8 Hz)

EXAMPLE 10

The following object compounds were obtained according to a similarmanner to that of Example 1.

(1) MASS (m/z): 595 (M+H)⁺ ; NMR (CDCl₃, δ): 2.25-2.45 (4H, m), 2.27(3H, s), 2.60-2.75 (1H, m), 2.80 (2/3×3H, s), 2.85 (1/3×3H, s),3.17-3.75 (5H, m), 4.29 (1/3×1H, d, J=17 Hz), 4.43 (1/3×1H, d, J=17 Hz),4.57 (2/3×1H, d, J=15 Hz), 4.72 (2/3×1H, d, J=15 Hz), 5.05-5.20 (1H, m),5.70-5.87 (1H m), 6.75-7.48 (14H, m), 7.58-7.70 (1H, m), 7.98-8.18 (1H,m), 8.35-8.45 (1H, m), 9.42 (1H, br s)

(2) MASS (m/z): 596 (M+H)⁺ ; NMR (CDCl₃, δ): 2.27 (3H, s), 2.30-2.48(4H, m), 2.65-2.80 (1H, m), 2.81 (2/3×3H, s), 2.85 (1/3×3H, s),3.20-3.70 (5H, m), 4.30 (1/3×1H, d, J=17 Hz), 4.45 (2/3×1H, d, J=15 Hz),4.58 (1/3×1H, d, J=17 Hz), 4.72 (2/3×1H, d, J=17 Hz), 5.04-5.18 (1H, m),5.77-5.88 (1H, m), 6.80-7.70 (15H, m), 8.12-8.50 (2H, m)

(3) MASS (m/z): 651 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28-2.52 (4H, m), 2.29(3H, s), 2.55-2.72 (1H, m), 2.58 (2/3×3H, s), 2.78 (1/3×3H, s), 2.92(6H, s), 2.95-3.10 (2H, m), 3.22-3.78 (5H, m), 3.98 (1/3×1H, d, J=17Hz), 4.20 (2/3×1H, d, J=15 Hz), 4.31 (1/3×1H, d, J=17 Hz), 4.57 (2/3×1H,d, J=15 Hz), 5.02-5.25 (2H, m), 6.47-8.12 (16H, m), 9.25-9.58 (1H, br s)

(4) MASS (m/z): 652 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.32-2.52(4H, m), 2.58 (2/3×3H, s), 2.60-2.72 (1H, m), 2.78 (1/3×3H, s), 2.92(6H, s), 2.96-3.10 (2H, m), 3.25-3.72 (5H, m), 3.98 (1/3×1H, d, J=17Hz), 4.21 (2/3×1H, d, J=15 Hz), 4.30 (1/3×1H, d, J=17 Hz), 4.54 (2/3×1H,d, J=15 Hz), 5.02-5.25 (2H, m), 6.58-7.75 (15H, m), 8.15-8.28 (1H, m)

(5) MASS (m/z): 666 (M+H)⁺ ; NMR (CDCl₃, δ): 2.22 (6H, s), 2.29 (3H, s),2.30-2.52 (4H, m), 2.55-2.70 (1H, m), 2.62 (2/3×3H, s), 2.82 (1/3×3H,s), 2.95-3.08 (2H, m), 3.22-3.78 (7H, m), 4.24 (1/3×2H, ABq, Δ=0.21,J=17 Hz), 4.29 (2/3×1H, d, J=15 Hz), 4.62 (2/3×1H, d, J=15 Hz),5.00-5.19 (2H, m), 6.90-8.13 (16H, m), 9.35 (1/3×1H, s), 9.42 (2/3×1H,s)

(6). MASS (m/z): 667 (M+H)⁺ ; NMR (CDCl₃, δ): 2.22 (6H, s), 2.30 (3H,s), 2.32-2.53 (4H, m), 2.59 (2/3×3H, s), 2.59-2.72 (1H, m), 2.80(1/3×3H, s), 2.94-3.12 (2H, m), 3.23-3.72 (7H, m), 4.22 (1/3×2H, ABq,Δ=0.19, J=17 Hz), 4.27 (2/3×1H, d, J=15 Hz), 4.63 (2/3×1H, d, J=15 Hz),5.00-5.20 (2H, m), 6.88-7.75 (15H, m), 8.15-8.25 (1H, m)

(7) MASS (m/z): 621 (M+H)⁺ ; NMR (CDCl₃, δ): 2.20-2.50 (4H, m), 2.28(3H, s), 2.55-2.82 (2H, m), 2.92-3.85 (10H, m), 3.98 (1/2×1H, d, J=17Hz), 4.48 (1/2×1H, d, J=17 Hz), 4.62 (1/2×2H, ABq, Δ=0.15, J=17 Hz),5.05-5.23 (2H, m), 6.80-8.15 (16H, m), 9.60 (1H, s)

(8) MASS (m/z): 622 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.55(4H, m), 2.55-3.82 (12H, m), 3.94 (2/5×1H, d, J=17 Hz), 4.48 (2/5×1H, d,J=17 Hz), 4.62 (3/5×2H, ABq, Δ=0.15, J=17 Hz), 5.02-5.23 (2H, m),6.80-7.82 (15H, m), 8.15-8.28 (1H, m)

(9) MASS (m/z): 643 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.53(4H, m), 2.58-2.70 (1H, m), 2.62 (3/4×3H, s), 2.78 (1/4×3H, s),2.97-3.10 (2H, m), 3.24-3.78 (5H, m), 4.20 (1/4×2H, ABq, Δ=0.16, J=17Hz), 4.25 (3/4×1H, d, J=15 Hz), 4.60 (3/4×1H, d, J=15 Hz), 5.02-5.17(2H, m), 6.80-8.13 (16H, m), 9.33 (1H, br s)

(10) MASS (m/z): 644 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.52(4H, m), 2.60 (3/4×3H, s), 2.60-2.72 (1H, m), 2.78 (1/4×3H, s),2.95-3.15 (2H, m), 3.25-3.74 (5H, m), 4.19 (1/4×2H, ABq, Δ=0.1S, J=17Hz), 4.24 (3/4×1H, d, J=15 Hz), 4.59 (3/4×1H, d, J=15 Hz), 5.02-5.18(2H, m), 6.80-7.01 (2H, m), 7.17-7.74 (13H, m), 8.13-8.28 (1H, m)

(11) MASS (m/z): 687, 689 (M+H)⁺ ; NMR (CDCl₃, δ): 2.25-2.52 (4H, m),2.30 (3H, s), 2.55-2.70 (1H, m), 2.62 (3/4×3H, s), 2.77 (1/4×3H, s),2.92-3.12 (2H, m), 3.22-3.38 (1H, m), 3.40-3.78 (4H, m), 4.20 (1/4×2H,ABq, Δ=0.15, J=17 Hz), 4.23 (3/4×1H, d, J=15 Hz), 4.59 (3/4×1H, d, J=15Hz), 5.03-5.18 (2H, m), 6.73-8.12 (16H, m), 9.43 (1H, br s)

(12) MASS (m/z): 688, 690 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s),2.30-2.52 (4H, m), 2.60-2.71 (1H, m), 2.62 (3/4×3H, s), 2.78 (1/4×3H,s), 2.95-3.17 (2H, m), 3.26-3.75 (5H, m), 4.17 (1/4×2H, ABq, Δ=0.14,J=17 Hz), 4.22 (3/4×1H, d, J=15 Hz), 4.58 (3/4×1H, d, J=15 Hz),5.02-5.18 (2H, m), 6.72-6.96 (2H, m), 7.10-7.72 (13H, m), 8.15-8.27 (1H,m) (13) MASS (m/z): 627 (M+H)⁺ ; NMR (CDCl₃, δ): 2.24-2.50 (4H, m), 2.28(3H, s), 2.60 (3/4×3H, s), 2.60-2.73 (1H, m), 2.78 (1/4×3H, s),2.93-3.13 (2H, m), 3.20-3.75 (5H, m), 4.20 (1/4×2H, ABq, Δ=0.17, J=17Hz), 4.21 (3/4×1H, d, J=15 Hz), 4.61 (3/4×1H, d, J=15 Hz), 5.06-5.21(2H, m), 6.82-8.12 (16H, m), 9.23 (1H, br s)

(14) MASS (m/z): 628 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.32-2.55(4H, m), 2.59 (3/4×3H, s), 2.60-2.72 (1H, m), 2.78 (1/4×3H, s),2.95-3.17 (2H, m), 3.26-3.75 (5H, m), 4.18 (1/4×2H, ABq, Δ=0.20, J=17Hz), 4.23 (3/4×1H, d, J=15 Hz), 4.59 (3/4×1H, d, J=15 Hz), 5.00-5.18(2H, m), 6.82-7.73 (15H, m), 8.15-8.27 (1H, m)

(15) MASS (m/z): 640 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.58(4H, m), 2.59 (3/4×3H, s), 2.60-2.70 (1H, m), 2.73 (1/4×3H, s),2.98-3.15 (2H, m), 3.20-3.35 (1H, m), 3.40-3.75 (4H, m), 3.92 (3H, s),3.95 (1/4×1H, d, J=17 Hz), 4.21 (3/4×1H, d, J=15 Hz), 4.26 (1/4×1H, d,J=17 Hz), 4.50 (3/4×1H, d, J=15 Hz), 5.02-5.25 (2H, m), 6.58-6.68 (1H,m), 6.95-8.13 (14H, m), 9.73 (1/4×1H, br s), 9.78 (3/4×1H, br s)

(16) MASS (m/z): 641 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.35-2.52(4H, m), 2.58 (3/4×3H, s), 2.60-2.72 (1H, m), 2.73 (1/4×3H, s),2.98-3.16 (2H, m), 3.28-3.40 (1H, m), 3.40-3.75 (4H, m), 3.92 (3H, s),3.95 (1/4×1H, d, J=17 Hz), 4.20 (3/4×1H, d, J=15 Hz), 4.26 (1/4×1H, d,J=17 Hz), 4.52 (3/4×1H, d, J=15 Hz), 5.00-5.25 (2H, m), 6.60-6.70 (1H,m), 7.03-8.25 (14H, m)

(17) MASS (m/z): 657 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.33-2.56(4H, m), 2.56-2.68 (1H, m), 2.60 (3/4×3H, s), 2.75 (1/4×3H, s),2.98-3.15 (2H, m), 3.25-3.42 (1H, m), 3.42-3.73 (4H, m), 3.91 (3H, s),3.94 (1/4×1H, d, J=17 Hz), 4.23 (3/4×1H, d, J=15 Hz), 4.28 (1/4×1H, d,J=17 Hz), 4.52 (3/4×1H, d, J=15 Hz), 4.98-5.21 (2H, m), 6.60-6.70 (1H,m), 7.05-8.18 (14H, m)

(18) MASS (m/z): 623 (M+H)⁺ ; NMR (CDCl₃, δ): 0.98 (3/5×3H, t, J=7 Hz),1.01 (2/5×3H, t, J=7 Hz), 2.25-2.74 (5H, m), 2.28 (3H, s), 2.92-3.18(4H, m), 3.22-3.38 (1H, m), 3.40-3.75 (4H, m), 4.17 (3/5×1H, d, J=15Hz), 4.19 (2/5×2H, ABq, Δ=0.18, J=17 Hz), 4.84 (3/5×1H, d, J=15 Hz),5.00-5.20 (2H, m), 6.95-8.10 (17H, m), 9.48 (2/5×1H, br s), 9.53(3/5×1H, br s)

(19) MASS (m/z): 624 (M+H)⁺ ; NMR (CDCl₃, δ): 0.97 (3/5×3H, t, J=7 Hz),1.00 (2/5×3H, t, J=7 Hz), 2.30 (3H, s), 2.30-2.72 (5H, m), 2.93-3.20(4H, m), 3.25-3.75 (5H, m), 4.17 (3/5×1H, d, J=15 Hz), 4.17 (2/5×2H,ABq, Δ=0.18, J=17 Hz), 4.81 (3/5×1H, d, J=15 Hz), 4.97-5.18 (2H, m),6.93-7.72 (16H, m), 8.15-8.27 (1H, m)

(20) MASS (m/z): 644 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28-2.55 (4H, m), 2.30(3H, s), 2.60-2.71 (1H, m), 2.64 (4/5×3H, s), 2.74 (1/5×3H, s),2.93-3.16 (2H, m), 3.21-3.35 (1H, m), 3.40-3.75 (4H, m), 4.18 (1/5×2H,ABq, Δ=0.21, J=17 Hz), 4.41 (4/5×2H, ABq, Δ=0.15, J=15 Hz), 5.02-5.17(2H, m), 6.95-8.20 (15H, m), 9.59 (1/5×1H, s), 9.68 (4/5×1H, s)

(21) MASS (m/z): 645 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.52(4H, m), 2.58-2.71 (1H, m), 2.62 (4/5×3H, s), 2.73 (1/5×3H, s),2.96-3.20 (2H, m), 3.25-3.40 (1H, m), 3.40-3.73 (4H, m), 4.20 (1/5×2H,ABq, Δ=0.19, J=17 Hz), 4.28 (4/5×1H, d, J=15 Hz), 4.54 (4/5×1H, d, J=15Hz), 5.02-5.15 (2H, m), 7.05-7.73 (13H, m), 8.02-8.25 (2H, m)

(22) MASS (m/z): 661 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.53(4H, m), 2.53-2.68 (1H, m), 2.63 (4/5×3H, s), 2.75 (1/5×3H, s),2.95-3.12 (2H, m), 3.26-3.40 (1H, m), 3.40-3.71 (4H, m), 4.20 (1/5×2H,ABq, Δ=0.24, J=17 Hz), 4.43 (4/5×2H, ABq, Δ=0.21, J=15 Hz ), 4 .98-5.12(2H, m), 7.10-8.20 (15H, m)

(23) MASS (m/z): 624 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.50(4H, m), 2.52 (1/5×3H, s), 2.55 (4/5×3H, s), 2.58-2.70 (1H, m), 2.61(4/5×3H, s), 2.75 (1/5×3H, s), 2.95-3.12 (2H, m), 3.23-3.36 (1H, m),3.41-3.75 (4H, m), 4.02 (1/5×1H, d, J=17 Hz), 4.32 (1/5×1H, d, J=17 Hz),4.41 (4/5×2H, ABq, Δ=0.12, J=15 Hz), 5.00-5.20 (2H, m), 6.96-8.31 (15H,m), 9.34 (1/5×1H, m), 9.61 (4/5×1H, s)

(24) MASS (m/z): 625 (M+H)⁺ ; NMR (CDCl₃ δ): 2.31 (3H, s), 2.32-2.50(4H, m), 2.53 (3H, s), 2.59 (3/4×3H, s), 2.60-2.71 (1H, m), 2.73(1/4×3H, s), 2.98-3.15 (2H, m), 3.25-3.73 (5H, m), 4.01 (1/4×1H, d, J=17Hz), 4.27 (3/4×1H, d, J=15 Hz), 4.30 (1/4×1H, d, J=17 Hz), 4.56 (3/4×1H,d, J=15 Hz), 5.02-5.20 (2H, m), 7.02-7.75 (13H, m), 8.15-8.30 (2H, m)

(25) MASS (m/z): 641 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s), 2.32-2.50(4H, m), 2.52 (3H, s), 2.57-2.69 (1H, m), 2.62 (3/4×3H, s), 2.76(1/4×3H, s), 2.98-3.14 (2H, m), 3.26-3.72 (5H, m), 4.02 (1/4×1H, d, J=17Hz), 4.30 (3/4×1H, d, J=15 Hz), 4.32 (1/4×1H, d, J=17 Hz), 4.56 (3/4×1H,d, J=15 Hz), 4.99-5.18 (2H, m), 7.02-8.31 (15H, m)

(26) MASS (m/z): 6.11 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53 (1/4×3H, s), 2.55(3/4×3H, s), 2.60-2.71 (1H, m), 2.62 (3/4×3H, s), 2.76 (1/4×3H, s),2.92-3.15 (2H, m), 3.18-3.35 (1H, m), 3.35-3.78 (8H, m), 4.02 (1/4×1H,d, J=17 Hz), 4.32 (1/4×1H, d, J=17 Hz), 4.42 (3/4×2H, ABq, Δ=0.15, J=15Hz), 5.02-5.22 (2H, m), 6.92-8.35 (15H, m), 9.62 (1/4×1H, s), 9.81(3/4×1H, s)

(27) MASS (m/z): 612 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52 (3H, s), 2.58-2.70(1H, m), 2.60 (3/4×3H, s), 2.75 (1/4×3H, s), 2.95-3.15 (2H, m),3.22-3.39 (1H, m), 3.39-3.80 (8H, m), 4.00 (1/4×1H, d, J=17 Hz), 4.29(3/4×1H, d, J=15 Hz), 4.31 (1/4×1H, d, J=17 Hz), 4.55 (3/4×1H, d, J=15Hz), 5.00-5.20 (2H, m), 7.00-7.78 (13H, m), 8.12-8.32 (2H, m)

(28) MASS (m/z): 628 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52 (3H, s), 2.55-2.68(1H, m), 2.62 (3/4×3H, s), 2.76 (1/4×3H, s), 2.95-3.14 (2H, m),3.22-3.38 (1H, m), 3.40-3.80 (8H, m), 4.02 (1/4×1H, d, J=17 Hz), 4.35(1/4×1H, d, J=17 Hz), 4.44 (3/4×2H, ABq, Δ=0.23, J=15 Hz), 4.98-5.18(2H, m), 7.00-8.33 (15H, m)

(29) MASS (m/z): 614 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.63(5H, m), 2.62 (3/4×3H, s), 2.82 (1/4×3H, s), 2.93-3.10 (2H, m),3.22-3.40 (1H, m), 3.40-3.75 (4H, m), 4.26 (1/4×2H, ABq, Δ=0.21, J=17Hz), 4.32 (1/4×1H, d, J=15 Hz), 4.64 (1/4×1H, d, J=15 Hz), 4.93-5.15(2H, m), 6.04 (2H, s), 6.80-7.98 (15H, m)

(30) MASS (m/z): 676 (M+H)⁺ ; NMR (CDCl₃, δ): 2.25-2.50 (4H, m), 2.28(3H, s), 2.60-2.72 (1H, m), 2.66 (2/3×3H, s), 2.80 (1/3×3H, s),2.92-3.16 (2H, m), 3.22-3.74 (5H, m), 4.27 (1/3×2H, ABq, Δ=0.18, J=17Hz), 4.49 (2/3×2H, ABq, Δ=0.22, J=15 Hz), 5.05-5.21 (2H, m), 6.95-7.88(15H, m), 8.01-8.13 (2H, m), 8.50 (2/3×1H, s), 8.52 (1/3×1H, s)

(31) MASS (m/z): 677 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.54(4H, m), 2.58-2.75 (1H, m), 2.67 (3/4×3H, s), 2.80 (1/4×3H, s),2.97-3.21 (2H, m), 3.28-3.77 (5H, m), 4.28 (1/4×2H, ABq, Δ=0.17, J=17Hz), 4.52 (3/4×2H, ABq, Δ=0.23, J=15 Hz), 5.02-5.22 (2H, m), 7.00-7.75(15H, m), 8.10 (3/4×1H, s), 8.18 (1/4×1H, s), 8.20-8.28 (1H, m), 8.52(3/4×1H, s), 8.53 (1/4×1H, s)

(32) MASS (m/z): 693 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s), 2.31-2.70(5H, m), 2.68 (3/4×3H, s), 2.81 (1/4×3H, s), 2.97-3.20 (2H, m),3.25-3.73 (5H, m), 4.31 (1/4×2H, ABq, Δ=0.21, J=17 Hz), 4.53 (3/4×2H,ABq, Δ=0.18, J=15 Hz), 4.98-5.20 (2H, m), 7.03-7.94 (15H, m), 8.05-8.21(2H, m), 8.52 (3/4×1H, s), 8.53 (1/4×1H, s)

(33) MASS (m/z): 644 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.52(4H, m), 2.58-2.70 (1H, m), 2.63 (4/5×3H, s), 2.78 (1/5×3H, s),2.95-3.10 (2H, m), 3.22-3.75 (5H, m), 4.21 (1/5×2H, ABq, Δ=0.24, J=17Hz), 4.43 (4/5×2H, ABq, Δ=0.20, J=15 Hz), 5.00-5.15 (2H, m), 6.93-8.18(13H, m), 8.27 (1H, s), 8.48 (1H, s), 9.39 (1/5×1H, s), 9.51 (4/5×1H, s)

(34) MASS (m/z): 645 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s), 2.31-2.52(4H, m), 2.60-2.72 (1H, m), 2.62 (4/5×3H, s), 2.78 (1/5×3H, s),2.98-3.17 (2H, m), 3.25-3.76 (5H, m), 4.21 (1/5×2H, ABq, Δ=0.22, J=17Hz), 4.30 (2/5×1H, d, J=15 Hz), 4.59 (2/5×1H, d, J=15 Hz), 5.00-5.18(2H, m), 7.10-7.85 (12H, m), 8.11-8.31 (2H, m), 8.48 (1H, s)

(35) MASS (m/z): 661 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s), 2.30-2.53(4H, m), 2.53-2.72 (1H, m), 2.65 (3/4×3H, s), 2.79 (1/4×3H, s),2.96-3.16 (2H, m), 3.25-3.76 (5H, m), 4.08 (1/4×1H, d, J=17 Hz), 4.32(3/4×1H, d, J=15 Hz), 4.34 (1/4×1H, d, J=17 Hz), 4.58 (3/4×1H, d, J=15Hz), 4.95-5.12 (2H, m), 7.10-7.97 (12H, m), 8.05-8.30 (2H, m), 8.49 (1H,s)

(36) MASS (m/z): 631 (M+H)⁺ ; NMR (CDCl₃, δ): 2.54-2.70 (1H, m), 2.66(4/5×3H, s), 2.73 (1/5×3H, s), 2.91-3.15 (2H, m), 3.15-3.32 (1H, m),3.32-3.76 (8H, m), 4.18 (1/5×2H, ABq, Δ=0.24, J=17 Hz), 4.41 (4/5×2H,ABq, Δ=0.15, J=15 Hz), 5.00-5.20 (2H, m), 6.92-8.20 (15H, m), 9.74(1/5×1H, s), 9.80 (4/5×1H, s)

(37) MASS (m/z): 632 (M+H)⁺ ; NMR (CDCl₃, δ): 2.58-2.72 (1H, m), 2.63(4/5×3H, s), 2.75 (1/5×3H, s), 2.94-3.20 (2H, m), 3.22-3.80. (9H, m),4.19 (1/5×2H, ABq, Δ=0.24, J=17 Hz), 4.42 (4/5×2H, ABq, Δ=0.22, J=15Hz), 5.01-5.18 (2H, m), 7.08-7.77 (13H, m), 8.02-8.26 (2H, m)

(38) MASS (m/z): 648 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52-2.70 (1H, m), 2.66(4/5×3H, s), 2.77 (1/5×3H, s), 2.93-3.18 (2H, m), 3.22-3.82 (9H, m),4.06 (1/5×1H, d, J=17 Hz), 4.32 (1/5×1H, d, J=17 Hz), 4.42 (2/5×2H, ABq,Δ=0.18, J=15 Hz), 4.97-5.15 (2H, m), 7.08-7.52 (9H, m), 7.65-7.93 (4H,m), 8.03-8.21 (2H, m)

(39) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.70 (1H, m), 2.68(4/5×3H, s), 2.79 (1/5×3H, s), 2.98-3.06 (2H, m), 3.22-3.33 (1H, m),3.40-3.78 (8H, m), 4.09 (1/5×1H, d, J=17 Hz), 4.36 (1/5×1H, d, J=17 Hz),4.48 (4/5×2H, ABq, Δ=0.15, J=15 Hz), 5.03-5.18 (2H, m), 6.95-7.48 (11H,m), 7.63-7.78 (2H, m), 8.00-8.12 (1H, m), 8.30-8.55 (2H, m), 9.33(1/5×1H, br s), 9.51 (4/5×1H, br s)

(40) MASS (m/z): 598 (M+H)⁺ ; NMR (CDCl₃, δ): 2.57-2.72 (1H, m), 2.62(3/4×3H, s), 2.77 (1/4×3H, s), 2.95-3.18 (2H, m), 3.22-3.81 (9H, m),4.09 (1/4×1H, d, J=17 Hz), 4.31 (3/4×1H, d, J=15 Hz), 4.34 (1/4×1H, d,J=17 Hz), 4.61 (3/4×1H, d, J=15 Hz), 5.02-5.19 (2H, m), 7.10-7.76 (13H,m), 8.13-8.25 (1H, m), 8.30 (1/4×1H, s), 8.38 (3/4×1H, s), 8.46-8.55(1H, m)

(41) MASS (m/z): 611 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s), 2.31-2.52(4H, m), 2.60-2.73 (1H, m), 2.62 (3/4×3H, s), 2.77 (1/4×3H, s),2.98-3.18 (2H, m), 3.27-3.77 (5H, m), 4.22 (1/4×2H, ABq, Δ=0.22, J=17Hz), 4.29 (3/4×1H, d, J=15 Hz), 4.62 (3/4×1H, d, J=15 Hz), 5.03-5.20(2H, m), 7.12-7.78 (13H, m), 8.16-8.25 (1H, m), 8.28 (1/4×1H, s), 8.38(3/4×1H, s), 8.48-8.55 (1H, m)

(42) MASS (m/z): 623 (M+H)⁺ ; NMR (CDCl₃, δ): 1.07 (3H, t, J=7 Hz),2.28-2.52 (6H, m), 2.61 (2/3×3H, s), 2.61-2.76 (1H, m), 2.81 (1/3×3H,s), 2.92-3.11 (2H, m), 3.18-3.35 (1H, m), 3.35-3.75 (4H, m), 4.26(2/3×1H, d, J=15 Hz), 4.27 (1/3×2H, ABq, Δ=0.22, J=17 Hz), 4.68 (2/3×1H,d, J=15 Hz), 5.04-5.22 (2H, m), 6.92-8.12 (17H, m), 9.68 (1/3×1H, s),9.72 (2/3×1H, s)

(43) MASS (m/z): 624 (M+H)⁺ ; NMR (CDCl₃, δ): 1.07 (3H, t, J=7 Hz),2.32-2.54 (6H, m), 2.58 (2/3×3H, s), 2.58-2.70 (1H, m), 2.80 (1/3×3H,s), 2.94-3.14 (2H, m), 3.24-3.74 (5H, m), 4.24 (1/3×2H, ABq, Δ=0.22,J=17 Hz), 4.28 (2/3×1H, d, J=15 Hz), 4.63 (2/3×1H, d, J=15 Hz),5.00-5.29 (2H, m), 6.90-7.74 (16H, m), 8.15-8.27 (1H, m)

(44) MASS (m/z): 640 (M+H)⁺ ; NMR (CDCl₃, δ): 1.08 (3H, t, J=7 Hz),2.32-2.58 (6H, m), 2.58-2.70 (1H, m), 2.62 (2/3×3H, s), 2.82 (1/3×3H,s), 2.93-3.13 (2H, m), 3.24-3.75 (5H, m), 4.28 (1/3×2H, ABq, Δ=0.22,J=17 Hz), 4.32 (2/3×1H, d, J=15 Hz), 4.65 (2/3×1H, d, J=15 Hz),4.95-5.18 (2H, m), 6.92-8.20 (17H, m)

(45) MASS (m/z): 640 (M⁺ +1); NMR (CDCl₃, δ): 2.29 (3H, s), 2.42 (4H,m), 2.57 (3H×2/3, s), 2.66 (1H, dd, J=6, 16 Hz), 2.77 (3H×1/3, s), 3.04(2H, m), 3.33 (1H, m), 3.49 (2H, m), 3.67 (2H, m), 3.77 (3H, s), 4.02(1H×1/3, d, J=16 Hz), 4.21 (1H×2/3, d, J=15 Hz), 4.29 (1H×1/3, d, J=16Hz), 4.57 (1H×2/3, d, J=15 Hz), 5.06-5.19 (2H, m), 6.80 (2H, d, J=8 Hz),6.87-7.02 (2H, m), 7.17-7.21 (5H, m), 7.31 (1H, t, J=8 Hz), 7.44 (1H, t,J=8 Hz), 7.51 (1H, s), 7.56 (1H, d, J=8 Hz), 7.64-7.72 (2H, m), 8.22(1H, m)

(46) MASS (ESI) (m/z): 640 (M+H)⁺ ; NMR (CDCl₃, δ): 2.27 (3H, s), 2.29(3H, s), 2.23-2.52 (4H, m), 2.55-2.68 (1H, m), 2.61 (3×2/3H, s), 2.80(3×1/3H, s), 2.97-3.10 (2H, m), 3.28-3.38 (1H, m), 3.42-3.58 (2H, m),3.62-3.72 (2H, m), 4.09 (2×1/4H, d, J=17 Hz), 4.27 (2×1/4H, d, J=15 Hz),4.33 (2×1/4H, d, J=17 Hz), 4.60 (2×1/4H, d, J=15 Hz), 4.99-5.15 (2H, m),6.89 (2×1/3H, d, J=8 Hz), 6.98 (2×2/3H, d, J=8 Hz), 7.07 (2H, d, J=8Hz), 7.12-7.20 (5H, m), 7.38-7.48 (2H, m), 7.71 (1H, t, J=8 Hz),7.80-7.88 (3H, m), 8.12 (1H, d, J=8 Hz)

(47) MASS (ESI) (m/z): 623 (M+H)⁺ ; NMR (CDCl₃, δ): 2.21 (3H, s), 2.27(3H, s), 2.28-2.40 (4H, m), 2.56 (3×2/3H, s), 2.62-2.78 (1H, m), 2.80(3×1/3H, s), 2.93-3.08 (2H, m), 3.18-3.27 (1H, m), 3.35-3.48 (2H, m),3.53-3.70 (2H, m), 4.13 (2×1/6H, d, J=17 Hz), 4.20 (2×1/3H, d, J=15 Hz),4.31 (2×1/6H, d, J=17 Hz), 4.68 (2×1/3H, d, J=15 Hz), 5.12-5.30 (2H, m),6.86 (2×1/3H, d, J=8 Hz), 6.93 (2×2/3H, d, J=8 Hz), 6.98-7.12 (9H, m),7.22 (1H, t, J=8 Hz), 7.44 (1H, d, J=8 Hz), 7.63 (1H, d, J=8 Hz),8.01-8.11 (2H, m)

(48) MASS (ESI) (m/z): 624 (M+H)⁺ ; NMR (CDCl₃, δ): 2.29 (3H, s), 2.31(3H, s), 2.33-2.52 (4H, m), 2.58 (3×2/3H, s), 2.61-2.71 (1H, m), 2.79(3×1/3H, s), 2.98-3.12 (2H, m), 3.28-3.38 (1H, m), 3.42-3.57 (2H, m),3.62-3.72 (2H, m), 4.08 (2×1/4H, d, J=17 Hz), 4.23 (2×1/4H, d, J=15 Hz),4.31 (2×1/4H, d, J=17 Hz), 4.61 (2×1/4H, d, J=15 Hz), 5.03-5.18 (2H, m),6.86 (2×1/3H, d, J=8 Hz), 6.97 (2×2/3H, d, J=8 Hz), 7.09 (2H, d, J=8Hz), 7.12-7.22 (5H, m), 7.29 (1H, t, J=8 Hz), 7.43 (1H, t, J=8 Hz), 7.49(1H, s), 7.58 (1H, d, J=8 Hz), 7.67 (2H, q, J=8 Hz), 8.20-8.23 (1H, m)

(49) MASS (m/z): 550 (M⁺ +1); NMR (CDCl₃, δ): 2.29 (3H, s), 2.39 (4H,m), 2.57-2.72 (1H, m), 2.89 (3H×1/3, s), 2.99 (3H×2/3, s), 3.38-3.51(3H, m), 3.54-3.70 (3H, m), 3.78 (1H, dd, J=5, 11 Hz), 3.87-3.98 (1H,m), 4.44 (1H×2/3, d, J=15 Hz), 4.63 (2H×1/3, s), 4.67 (1H×2/3, d, J=15Hz), 5.03 (1H, m), 5.09 (1H×1/3, m), 5.16 (1H×2/3, m), 7.16-7.19 (2H,m), 7.25-7.37 (4H, m), 7.44 (1H, t, J=8 Hz), 7.53 (1H, s), 7.58 (1H, d,J=8 Hz), 7.67 (1H, d, J=8 Hz), 7.74 (1H, d, J=8 Hz), 8.06 (1H, m)

(50) MASS (m/z): 576 (M⁺ +1); NMR (CDCl₃, δ): 0.79 (3H×1/3, d, J=7 Hz),0.83 (3H×1/3, d, J=7 Hz), 0.93 (3H×2/3, d, J=7 Hz), 0.96 (3H×2/3, d, J=7Hz), 1.38-1.49 (1H, m), 1.58-1.75 (2H, m), 2.27 (3H, s), 2.38 (4H, m),2.65 (1H, m), 2.89 (3H×1/3, s), 2.97 (3H×2/3, s), 3.29 (1H, dd, J=3, 16Hz), 3.46 (2H, m), 3.65 (2H, m), 4.36 (1H×2/3, d, J=15 Hz), 4.60(1H×1/3, d, J=15 Hz), 4.65 (1H×1/3, d, J=15 Hz), 4.73 (1H×2/3, d, J=15Hz), 4.96 (1H, m), 5.11 (1H, m), 7.16-7.36 (5H, m), 7.41 (2H, t, J=8Hz), 7.48 (1H, s), 7.53 (1H, d, J=8 Hz), 7.59-7.73 (2H, m), 8.24 (1H, d,J=8 Hz)

(51) MASS (m/z): 678 (M⁺ +1); NMR (CDCl₃, δ): 2.30 (3H, s), 2.42 (4H,m), 2.64 (3H×3/4, s), 2.67 (1H, dd, J=7, 16 Hz), 2.80 (3H×1/4, s),2.96-3.15 (2H, m), 3.34 (1H, dd, J=3, 16 Hz), 3.49 (2H, m), 3.67 (2H,m), 4.27 (1H×1/4, d, J=16 Hz), 4.34 (1H×1/4, d, J=16 Hz), 4.36 (1H×3/4,d, J=15 Hz), 4.66 (1H×3/4, d, J=15 Hz), 5.02-5.18 (2H, m), 6.99-7.21(7H, m), 7.30 (1H, t, J=8 Hz), 7.44 (1H, t, J=8 Hz), 7.51-7.62 (4H, m),7.67-7.71 (2H, m), 8.21 (1H, t, J=8 Hz)

(52) MASS (m/z): 677 (M⁺ +1); NMR (CDCl₃, δ): 2.24 (3H, s), 2.30-2.39(4H, m), 2.63 (3H×3/4, s), 2.71 (1H, dd, J=5, 16 Hz), 2.78 (3H×1/4, s),2.93-3.12 (2H, m), 3.25 (1H, dd, J=3, 16 Hz), 3.43 (2H, m), 3.62 (2H,m), 4.27 (1H×3/4, d, J=15 Hz), 4.32 (2H×1/4, s), 4.67 (1H×3/4, d, J=15Hz), 5.06-5.25 (2H, m), 6.96-7.28 (10H, m), 7.43-7.49 (3H, m), 7.65 (1H,d, J=8 Hz), 8.03 (1H, d, J=7 Hz), 8.10 (1H, d, J=7 Hz)

(53) MASS (m/z): 610 (M⁺ +1); NMR (CDCl₃, δ): 2.28 (3H, s), 2.37-2.40(4H, m), 2.52 (1H, dd, J=7, 16 Hz), 2.64 (3H×2/3, s), 2.88 (3H×1/3, s),2.97-3.09 (2H, m), 3.17 (1H×1/3, dd, J=3, 16 Hz), 3.28 (1H×2/3, dd, J=3,16 Hz), 3.37-3.48 (2H, m), 3.56-3.74 (2H, m), 4.28 (1H×2/3, d, J=15 Hz),4.29 (1H×1/3, d, J=15 Hz), 4.41 (1H×1/3, d, J=15 Hz), 4.72 (1H×2/3, d,J=15 Hz), 4.94 (1H×1/3, dt, J=4, 7 Hz), 5.10 (1H×2/3, dt, J=4, 7 Hz),5.19 (1H, dt, J=7, 7 Hz), 7.02 (1H, d, J=7 Hz), 7.07-7.32 (10H, m), 7.42(1H, t, J=8 Hz), 7.48-7.55 (2H, m), 7.66 (1H, d, J=8 Hz), 7.84 (1H×2/3,d, J=8 Hz), 7.92 (1H×1/3, d, J=8 Hz), 8.00 (1H×1/3, d, J=8 Hz), 8.16(1H×2/3, d, J=8 Hz)

(54) MASS (m/z): 610 (M⁺ +1); NMR (CDCl₃, δ): 2.27 (3H, s), 2.37-2.43(4H, m), 2.58 (3H×2/3, s), 2.66 (1H, dd, J=7, 15 Hz), 2.79 (3H×1/3, s),3.04 (2H, m), 3.29 (1H, dt, J=4, 15 Hz), 3.47 (2H, m), 3.65 (2H, m),4.14 (1H×1/3, d, J=15 Hz), 4.26 (1H×2/3, d, J=15 Hz), 4.33 (1H×1/3, d,J=15 Hz), 4.63 (1H×2/3, d, J=15 Hz), 5.02-5.16 (2H, m), 6.92-7.05 (2H,m), 7.15 (5H, m), 7.23-7.30 (4H, m), 7.42 (1H, t, J=8 Hz), 7.48 (1H, s),7.54 (1H, d, J=8 Hz), 7.64-7.74 (2H, m), 8.22 (1H, m)

(55) MASS (m/z): 610 (M⁺ +1); NMR (CDCl₃, δ): 2.28 (3H, s), 2.37-2.40(4H, m), 2.52 (1H, dd, J=7, 16 Hz), 2.64 (3H×2/3, s), 2.88 (3H×1/3, s),2.97-3.09 (2H, m), 3.17 (1H×1/3, dd, J=3, 16 Hz), 3.28 (1H×2/3, dd, J=3,16 Hz), 3.37-3.48 (2H, m), 3.56-3.74 (2H, m), 4.28 (1H×2/3, d, J=15 Hz),4.29 (1H×1/3, d, J=15 Hz), 4.41 (1H×1/3, d, J=15 Hz), 4.72 (1H×2/3, d,J=15 Hz), 4.94 (1H×1/3, dt, J=4, 7 Hz), 5.10 (1H×2/3, dt, J=4, 7 Hz),5.19 (1H, dt, J=7, 7 Hz), 7.02 (1H, d, J=7 Hz), 7.07-7.32 (10H, m), 7.42(1H, t, J=8 Hz), 7.48-7.55 (2H, m), 7.66 (1H, d, J=8 Hz), 7.84 (1H×2/3,d, J=8 Hz), 7.92 (1H×1/3, d, J=8 Hz), 8.00 (1H×1/3, d, J=8 Hz), 8.16(1H×2/3, d, J=8 Hz)

(56) MASS (FAB) (m/z): 598 (M+H)⁺ ; NMR (CDCl₃, δ): 2.67 (3×2/3H, s),2.68-2.74 (1H, m), 2.83 (3×1/3H, s), 2.98-3.12 (2H, m), 3.20-3.31 (1H,m), 3.39-3.53 (2H, m), 3.60-3.75 (6H, m), 4.13-4.42 (2×2/3H, m), 4.63(2×1/3H, d, J=15 Hz), 5.07-5.20 (2H, m), 6.99-7.08 (2H, m), 7.12-7.33(9H, m), 7.49 (1H, s), 7.67 (1H, t, J=8 Hz), 8.03 (1H, d, J=8 Hz), 8.23(1H, d, J=8 Hz), 8.48 (1H, d, J=5 Hz)

(57) MASS (FAB) (m/z): 643 (M+H)⁺ ; NMR (CDCl₃, δ): 2.59-2.70 (1H, m),2.65 (3×2/3H, s), 2.82 (3×1/3H, s), 2.98-3.07 (2H, m), 3.21-3.33 (1H,m), 3.40-3.53 (2H, m), 3.62-3.75 (6H, m), 4.11-4.46 (2×2/3H, m), 4.62(2×1/3H, d, J=15 Hz), 5.02-5.17 (2H, m), 7.01-7.35 (10H, m), 7.63 (1H,s), 7.67 (1H, d, J=8 Hz), 8.40 (1H, d, J=8 Hz), 8.90 (1H, s), 9.38 (1H,s)

(58) MASS (FAB) (m/z): 645 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53-2.63 (1H, m),2.67 (3×2/3H, s), 2.83 (3×1/3H, s), 2.97-3.11 (2H, m), 3.30 (1H, t, J=15Hz), 3.42-3.59 (2H, m), 3.62-3.80 (6H, m), 4.13-4.45 (2×2/3H, m), 4.22(2H, s), 4.63 (2×1/3H, d, J=15 Hz), 5.08-5.18 (2H, m), 7.00-7.32 (11H,m), 7.35 (1H, t, J=8 Hz), 7.47 (1H, t, J=8 Hz), 7.53-7.62 (2H, m),7.70-7.83 (1H, m), 7.93 (1H, d, J=8 Hz), 8.06-8.11 (1H, m)

(59) MASS (FAB) (m/z): 627 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s),2.36-2.49 (4H, m), 2.62 (3×2/3H, s), 2.66-2.78 (1H, m), 2.81 (3×1/3H,s), 2.98-3.12 (2H, m), 3.28-3.37 (1H, m), 3.42-3.55 (2H, m), 3.66-3.71(2H, m), 4.13-4.40 (2×2/3H, m), 4.63 (2×1/3H, d, J=15 Hz), 5.02-5.20(2H, m), 6.97-7.08 (2H, m), 7.16-7.22 (5H, m), 7.26-7.31 (3H, m),7.48-7.73 (3H, m), 7.98 (1H, d, J=8 Hz), 8.15 (1H, d, J=8 Hz), 8.80-8.84(1H, m)

(60) MASS (FAB) (m/z): 644 (M+H)⁺ ; NMR (CDCl₃, δ): 2.29 (3H, s),2.36-2.49 (4H, s), 2.60 (3×2/3H, s), 2.58-2.70 (1H, m), 2.82 (3×1/3H,s), 2.97-3.11 (2H, m), 3.31 (1H, t, J=15 Hz), 3.42-3.58 (2H, m),3.66-3.72 (2H, m), 4.10-4.39 (2×2/3H, m), 4.65 (2×1/3H, d, J=15 Hz),5.01-5.18 (2H, m), 6.97-7.08 (2H, m), 7.12-7.21 (5H, m), 7.23-7.30 (3H,m), 7.39-7.52 (3H, m), 7.65 (1H, s), 7.72 (1H, d, J=8 Hz), 8.27 (1H, d,J=8 Hz)

(61) MASS (FAB) (m/z): 640 (M+H)⁺ ; NMR (CDCl₃, δ): 2.27 (3H, s),2.33-2.49 (4H, m), 2.58-2.71 (1H, m), 2.59 (3×2/3H, s), 2.80 (3×1/3H,s), 2.98-3.12 (2H, m), 3.29 (1H, t, J=15 Hz), 3.42-3.55 (2H, m),3.63-3.70 (2H, m), 3.84 (3H, s), 4.08-4.38 (2×2/3H, m), 4.65 (2×1/3H, d,J=15 Hz), 5.02-5.18 (2H, m), 6.94-7.08 (4H, m), 7.12-7.21 (5H, m),7.23-7.30 (3H, m), 7.43 (1H, s), 7.45 (1H, d, J=8 Hz), 7.65 (1×1/3H, d,J=8 Hz), 7.71 (1×2/3H, d, J=8 Hz), 8.15-8.20 (1H, m)

(62) MASS (FAB) (m/z): 688 (M+H)⁺ ; NMR (CDCl₃, δ): 2.30 (3H, s),2.36-2.50 (4H, m), 2.58-2.70 (1H, m), 2.62 (3×2/3H, s), 2.82 (3×1/3H,s), 2.98-3.12 (2H, m), 3.32 (1H, t, J=15 Hz), 3.42-3.57 (2H, m),3.63-3.71 (2H, m), 4.11-4.39 (2×2/3H, m), 4.65 (2×1/3H, d, J=15 Hz),5.00-5.18 (2H, m), 6.97-7.08 (2H, m), 7.13-7.21 (4H, m), 7.23-7.32 (4H,m), 7.40-7.53 (2H, m), 7.63-7.96 (2H, m), 8.20-8.22 (2H, m)

(63) MASS (FAB) (m/z): 640 (M+H)⁺ ; NMR (CDCl₃, δ): 2.29 (3H, s),2.35-2.47 (4H, m), 2.61 (3×2/3H, s), 2.71 (1H, dd, J=15, 8 Hz), 2.83(3×1/3H, s), 2.97-3.11 (2H, m), 3.19-3.29 (1H, m), 3.40-3.55 (2H, m),3.63-3.72 (2H, m), 4.02 (3H, s), 4.17-4.40 (2×2/3H, m), 4.67 (2×1/3H, d,J=15 Hz), 5.02-5.15 (2H, m), 6.90 (1H, d, J=8 Hz), 6.97 (1H, d, J=8 Hz),7.07 (1H, d, J=8 Hz), 7.12-7.21 (6H, m), 7.22-7.31 (4H, m), 7.48 (1H,s), 7.68 (1×1/3H, d, J=8 Hz), 7.75 (1×2/3H, d, J=8 Hz), 8.11 (1H, t, J=8Hz)

(64) MASS (FAB) (m/z): 563 (M+H)⁺ ; NMR (CDCl₃, δ): 2.50-2.71 (1H, m),2.62 (3×2/3H, s), 2.82 (3×1/3H, s), 2.99-3.06 (2H, m), 3.28 (1H, t, J=15Hz), 3.40-3.58 (2H, m), 3.62-3.79 (6H, m), 4.12-4.42 (2×2/3H, m), 4.65(2×1/3H, d, J=15 Hz), 4.95-5.13 (2H, m), 6.98-7.33 (11H, m), 7.51-7.71(3H, m), 7.90 (1H, t, J=8 Hz)

(65) MASS (FAB) (m/z): 547 (M+H)⁺ ; NMR (CDCl₃, δ): 2.51-2.58 (1H, m),2.59 (3×2/3H, s), 2.82 (3×1/3H, s), 3.00-3.10 (2H, m), 3.29 (1H, t, J=15Hz), 3.40-3.55 (2H, m), 3.63-3.76 (6H, m), 4.09-4.39 (2×2/3H, m), 4.64(2×1/3H, d, J=15 Hz), 4.98-5.17 (2H, m), 6.51-6.54 (1H, m), 6.93-7.32(11H, m), 7.51 (1H, s), 7.58 (1H, dd, J=18, 8 Hz), 7.99 (1H, d, J=8 Hz)

(66) MASS (FAB) (m/z): 558 (M+H)⁺ ; NMR (CDCl₃, δ): 2.59 (3×2/3H, s),2.61-2.72 (1H, m), 2.77 (3×1/3H, s), 2.99-3.05 (2H, m), 3.22-3.33 (1H,m), 3.41-3.55 (2H, m), 3.62-3.72 (6H, m), 4.12-4.45 (2×2/3H, m), 4.63(2×1/3H, d, J=15 Hz), 5.02-5.18 (2H, m), 6.92-7.22 (7H, m), 7.23-7.31(3H, m), 7.42-7.56 (2H, m), 7.88 (1H, t, J=8 Hz), 8.20 (1H, d, J=8 Hz),8.62 (1H, d, J=5 Hz), 9.18 (1H, d, J=8 Hz)

(67) MASS (FAB) (m/z): 556 (M+H)⁺ ; NMR (CDCl₃, δ): 2.49-2.68 (1H, m),2.65 (3×2/3H, s), 2.82 (3×1/3H, s), 2.98-3.05 (2H, m), 3.29 (1H, t, J=15Hz), 3.41-3.59 (2H, m), 3.61-3.78 (6H, m), 4.12-4.42 (2×2/3H, m), 4.65(2×1/3H, d, J=15 Hz), 5.00-5.13 (2H, m), 6.99-7.23 (7H, m), 7.25-7.32(3H, m), 7.43-7.57 (3H, m), 7.62-7.72 (1H, m), 7.85 (2H, d, J=8 Hz),8.07 (1H, t, J=8 Hz)

(68) MASS (FAB) (m/z): 495 (M+H)⁺ ; NMR (CDCl₃, δ): 2.03 (3H, d, J=5Hz), 2.43-2.55 (1H, m), 2.58 (3×2/3H, s), 2.82 (3×1/3H, s), 3.01 (2H, t,J=8 Hz), 3.18 (1H, t, J=8 Hz), 3.38-3.51 (2H, m), 3.58-3.63 (2H, m),3.67-3.75 (4H, m), 4.08 (2×1/8H, d, J=15 Hz), 4.28-4.38 (2×4/8H, m),4.63 (2×3/8H, d, J=15 Hz), 4.78-4.90 (1H, m), 5.01-5.12 (1H, m), 6.97(1H, d, J=8 Hz), 7.05-7.31 (10H, m), 7.53 (1H, t, J=8 Hz)

(69) MASS (FAB) (m/z): 608 (M+H)⁺ ; NMR (CDCl₃, δ): 2.60 (3×2/3H, s),2.68-2.88 (1H, m), 2.80 (3×1/3H, s), 3.05 (2H, t, J=8 Hz), 3.12-3.33(1H, m), 3.41-3.52 (2H, m), 3.62-3.73 (6H, m), 4.15-4.33 (2×2/3H, m),4.65 (2×1/3H, d, J=15 Hz), 5.10-5.21 (2H, m), 6.96-7.08 (2H, m),7.12-7.21 (5H, m), 7.23-7.31 (4H, m), 7.58-7.68 (2H, m), 7.80 (1H, t,J=8 Hz), 7.90 (1H, d, J=8 Hz), 8.21-8.35 (3H, m)

(70) MASS (FAB) (m/z): 546 (M+H)⁺ ; NMR (CDCl₃, δ): 2.50-2.62 (1H, m),2.61 (3×2/3H, s), 2.82 (3×1/3H, s), 2.96-3.08 (2H, m), 3.20-3.33 (1H,m), 3.43-3.50 (2H, m), 3.60-3.75 (6H, m), 4.11-4.40 (2×2/3H, m), 4.67(2×1/3H, d, J=15 Hz), 4.98-5.15 (2H, m), 6.13-6.17 (1H, m), 6.67-6.71(1H, m), 6.93-7.10 (3H, m), 7.12-7.32 (8H, m), 7.58-7.70 (2H, m), 9.48(1H, br s)

(71) MASS (FAB) (m/z): 607 (M+H)⁺ ; NMR (CDCl₃, δ): 2.62 (3×2/3H, s),2.67-2.75 (1H, m), 2.82 (3×1/3H, s), 3.02-3.09 (2H, m), 3.29-3.78 (9H,m), 4.08-4.43 (2×2/3H, m), 4.63 (2×1/3H, d, J=15 Hz), 5.08-5.22 (2H, m),7.00-7.33 (7H, m), 7.25-7.32 (3H, m), 7.43-7.96 (8H, m), 8.40 (1H, d,J=8 Hz)

(72) MASS (FAB) (m/z): 607 (M+H)⁺ ; NMR (CDCl₃, δ): 2.56-2.70 (1H, m),2.65 (3×2/3H, s), 2.83 (3×1/3H, s), 2.93-3.12 (2H, m), 3.31 (1H, t, J=15Hz), 3.43-3.58 (2H, m), 3.62-3.80 (6H, m), 4.15-4.45 (2×2/3H, m), 4.64(2×1/3H, d, J=15 Hz), 5.08-5.19 (2H, m), 7.01-7.22 (8H, m), 7.23-7.43(2H, m), 7.52-7.62 (2H, m), 7.73-7.83 (1H, m), 7.89-7.92 (3H, m), 7.98(1H, d, J=8 Hz), 8.22 (1H, d, J=8 Hz), 8.39 (1H, s)

(73) MASS (FAB) (m/z): 614 (M+H)⁺ ; NMR (CDCl₃, δ): 263 (3×2/3H, s),2.64-2.78 (1H, m), 2.81 (3×1/3H, s), 2.97-3.12 (2H, m), 3.22-3.32 (1H,m), 3.40-3.55 (2H, m), 3.60-3.76 (6H, m), 4.12-4.39 (2×2/3H, m), 4.63(2×1/3H, d, J=15 Hz), 5.01-5.18 (2H, m), 6.97-7.20 (7H, m), 7.23-7.30(3H, m), 7.47-7.71 (3H, m), 7.97 (1H, d, J=8 Hz), 8.15 (1H, d, J=8 Hz),8.82 (1H, d, J=8 Hz)

(74) MASS (FAB) (m/z): 659 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53-2.62 (1H, m),2.69 (2H, s), 2.82 (1H, s), 2.94-3.11 (2H, m), 3.26 (1H, t, J=15 Hz),3.42-3.58 (2H, m), 3.62-3.78 (6H, m), 4.12-4.48 (2×2/3H, m), 4.64(2×1/3H, d, J=15 Hz), 5.01-5.15 (2H, m), 7.01-7.22 (7H, m), 7.23-7.40(5H, m), 7.52-7.60 (2H, m), 7.70 (1H, d, J=8 Hz), 7.78 (1H, d, J=8 Hz),7.99-8.05 (2H, m), 8.12 (1H, d, J=8 Hz)

(75) MASS (FAB) (m/z): 598 (M+H)⁺ ; NMR (CDCl₃, δ): 2.60 (3×2/3H, s),2.52-2.72 (1H, m), 2.80 (3×1/3H, s), 2.94-3.10 (2H, m), 3.28 (1H, t,J=15 Hz), 3.40-3.52 (2H, m), 3.62-3.76 (6H, m), 4.12-4.42 (2×2/3H, m),4.62 (2×1/3H, d, J=15 Hz), 5.01-5.16 (2H, m), 6.98-7.18 (7H, m),7.22-7.32 (3H, m), 7.41-7.52 (2H, m), 7.65 (1H, d, J=8 Hz), 7.72 (1H, d,J=8 Hz), 7.85 (1H, d, J=8 Hz), 8.82 (1H, d, J=8 Hz)

(76) MASS (FAB) (m/z): 645 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28-2.42 (1H, m),2.53 (3×2/3H, s), 2.81 (3×1/3H, s), 2.82-3.01 (3H, m), 3.27-3.38 (2H,m), 3.43-3.70 (6H, m), 4.03-4.35 (2×2/3H, m), 4.62 (2×1/3H, d, J=15 Hz),4.75-4.88 (2H, m), 4.93-5.00 (1H, m), 6.90-6.98 (1H, m), 7.03-7.30 (12H,m), 7.32-7.55 (4H, m), 7.70-7.81 (3H, m)

(77) MASS (FAB) (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 2.65 (3×2/3H, s),2.83 (3×1/3H, s), 2.81-3.18 (4H, m), 3.40-3.47 (2H, m), 3.55-3.65 (6H,m), 4.28 (2×2/3H, t, J=15 Hz), 4.75 (2×1/3H, d, J=15 Hz), 5.20-5.30 (1H,m), 5.46-5.61 (1H, m), 6.93-7.11 (7H, m), 7.21-7.32 (5H, m), 7.46-7.52(1H, m), 7.78-7.83 (1H, m), 8.40-8.49 (1H, m), 8.63-8.72 (1H, m)

(78) MASS (FAB) (m/z): 615 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53 (3×2/3H, s),2.75 (3×1/3H, s), 2.80-2.92 (1H, m), 3.00-3.13 (2H, m), 3.25 (1H, dd,J=15, 4 Hz), 3.43-3.51 (2H, m), 3.60-3.69 (6H, m), 3.99-4.30 (2×2/3H,m), 4.58 (2×1/3H, d, J=15 Hz), 4.81-4.92 (1H, m), 5.13-5.20 (1H, m),6.83-6.97 (2H, m), 7.08-7.23 (10H, m), 7.35 (1H, d, J=8 Hz), 7.83-7.90(1H, m), 8.17 (1H, d, J=8 Hz)

(79) MASS (FAB) (m/z): 608 (M+H)⁺ ; NMR (CDCl₃, δ): 2.60-2.73 (1H, m),2.63 (3×2/3H, s), 2.81 (3×1/3H, s), 3.00-3.08 (2H, m), 3.30 (1H, t, J=15Hz), 3.41-3.56 (2H, m), 3.60-3.78 (6H, m), 4.09-4.47 (2×2/3H, m), 4.63(2×1/3H, d, J=15 Hz), 5.08-5.20 (2H, m), 7.00-7.33 (10H, m), 7.43-7.52(1H, m), 7.67-7.83 (2H, m), 7.88-8.03 (1H, m), 8.20 (1H, d, J=8 Hz),8.31 (1H, d, J=8 Hz), 8.58 (1H, s), 8.82-9.00 (1H, m)

(80) MASS (FAB) (m/z): 609 (M+H)⁺ ; NMR (CDCl₃, δ): 2.63 (3×2/3H, s),2.81 (3×1/3H, s), 2.68-2.80 (1H, m), 3.01-3.08 (2H, m), 3.23-3.35 (1H,m), 3.40-3.57 (2H, m), 3.63-3.75 (6H, m), 4.10-4.42 (2×2/3H, m), 4.63(2×1/3H, d, J=15 Hz), 5.11-5.22 (2H, m), 6.99-7.22 (6H, m), 7.24-7.32(4H, m), 7.62-7.72 (1H, m), 7.83-7.92 (2H, m), 8.12 (2H, t, J=8 Hz),9.11-9.17 (1H, m), 9.64 (1H, s)

(81) MASS (FAB) (m/z): 610 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.67 (1H, m),2.61 (3×2/3H, s), 2.81 (3×1/3H, s), 2.99-3.06 (2H, m), 3.27 (1H, t, J=15Hz), 3.40-3.58 (2H, m), 3.62-3.77 (6H, m), 4.03 (3H, s), 4.12-4.42(2×2/3H, m), 4.63 (2×1/3H, d, J=15 Hz), 4.99-5.17 (2H, m), 6.98-7.41(14H, m), 7.6i (2H, q, J=8 Hz), 8.01 (1H, t, J=8 Hz)

(82) MASS (FAB) (m/z): 7.40 (M+H)⁺ ; NMR (CDCl₃, δ): 1.23 (3H, t, J=8Hz), 2.52-2.71 (5H, m), 2.62 (3×2/3H, s), 2.79 (3×1/3H, s), 2.97-3.14(2H, m), 3.22 (2H, s), 3.28-3.39 (1H, m), 3.47-3.62 (2H, m), 3.68-3.78(2H, m), 3.91 (3H, s), 4.18 (2H, q, J=8 Hz), 4.30-4.38 (2×2/3H, m), 4.70(2×1/3H, d, J=15 Hz), 5.03-5.19 (2H, m), 6.97 (2×1/3H, d, J=8 Hz), 7.08(2×2/3H, d, J=8 Hz), 7.13-7.23 (5H, m), 7.30 (1H, t, J=8 Hz), 7.43 (1H,t, J=8 Hz), 7.49 (1H, s), 7.53-7.63 (1H, m), 7.69 (2H, t, J=8 Hz), 7.92(2H, d, J=8 Hz), 8.20 (1H, t, J=8 Hz)

(83) MASS (FAB) (m/z): 774 (M+H)⁺ ; NMR (CDCl₃, δ): 1.25 (3H, t, J=8Hz), 2.52-2.69 (5H, m), 2.62 (3×2/3H, s), 2.79 (3×1/3H, s), 2.97-3.11(2H, m), 3.20 (2H, s), 3.31 (1H, t, J=8 Hz), 3.43-3.60 (2H, m),3.68-3.77 (2H, m), 3.91 (3H, s), 4.18 (2H, q, J=8 Hz), 4.22-4.38(2×2/3H, m), 4.69 (2×1/3H, d, J=16 Hz), 5.01-5.18 (2H, m), 6.98 (2×1/3H,d, J=8 Hz), 7.08 (2×2/3H, d, J=8 Hz), 7.12-7.24 (5H, m), 7.40 (2H, t,J=8 Hz) 7.50 (1H, d, J=8 Hz), 7.60-7.70 (2H, m), 7.92 (2H, d, J=8 Hz),8.23 (1H, t, J=8 Hz)

(84) MASS (FAB) (m/z): 756 (M+H)⁺ ; NMR (CDCl₃, δ): 1.25 (3H, t, J=8Hz), 2.57-2.68 (5H, m), 2.63 (3×2/3H, s), 2.80 (3×1/3H, s), 2.97-3.11(2H, m), 3.22 (2H, s), 3.32 (1H, t, J=8 Hz), 3.47-3.63 (2H, m),3.68-3.75 (2H, m), 3.90 (3H, s), 4.18 (2H, q, J=8 Hz), 4.22-4.41(2×2/3H, m), 4.70 (2×1/3H, d, J=15 Hz), 5.00-5.18 (2H, m), 7.00 (2×1/3H,d, J=8 Hz), 7.09 (2×2/3H, d, J=8 Hz), 7.11-7.23 (5H, m), 7.38-7.47 (2H,m), 7.69 (1×1/3H, d, J=8 Hz), 7.73 (1×2/3H, d, J=8 Hz), 7.80-7.89 (3H,m), 7.93 (2H, d, J=8 Hz), 8.10-8.15 (1H, m)

(85) MASS (FAB) (m/z): 739 (M+H)⁺ ; NMR (CDCl₃, δ): 1.21 (3H, t, J=8Hz), 2.43-2.58 (4H, m), 2.63 (3×2/3H, s), 2.67-2.74 (1H, m), 2.80(3×1/3H, s), 2.92-3.10 (2H, m), 3.16 (2H, s), 3.21 (1H, t, J=8 Hz),3.40-3.52 (2H, m), 3.58-3.73 (2H, m), 3.90 (3H, s), 4.14 (2H, q, J=8Hz), 4.28 (2×1/2H, d, J=8 Hz), 4.73 (2×1/2H, d, J=15 Hz), 5.08-5.28 (2H,m), 6.92-7.16 (8H, m), 7.27 (2H, t, J=8 Hz), 7.43 (1H, d, J=8 Hz), 7.63(1H, d, J=8 Hz), 7.89 (2H, d, J=8 Hz), 8.01-8.10 (2H, m)

(86) MASS (FAB) (m/z): 716 (M+H)⁺ ; NMR (CDCl₃, δ): 1.23 (3H, t, J=8Hz), 2.53-2.70 (5H, m), 2.62 (3×2/3H, s), 2.81 (3×1/3H, s), 2.97-3.11(2H, m), 3.23 (2H, s), 3.31 (1H, t, J=15 Hz), 3.43-3.60 (2H, m),3.68-3.73 (2H, m), 4.11-4.38 (2×2/3H, m), 4.18 (2H, q, J=8 Hz), 4.65(2×1/3H, d, J=8 Hz), 5.02-5.17 (2H, m), 6.97 (2×1/3H, d, J=8 Hz), 7.04(2×2/3H, d, J=8 Hz), 7.11-7.21 (5H, m), 7.23-7.30 (3H, m), 7.37-7.51(3H, m), 7.63 (1H, s), 7.64 (1×1/3H, d, J=8 Hz), 7.71 (1×2/3H, d, J=8Hz), 8.21-8.27 (1H, m)

(87) MASS (FAB) (m/z): 698 (M+H)⁺ ; NMR (CDCl₃, δ): 1.26 (3H, t, J=8Hz), 2.56-2.69 (5H, m), 2.63 (3×2/3H, s), 2.83 (3×1/3H, s), 2.97-3.12(2H, m), 3.12 (2H, s), 3.31 (1H, t, J=15 Hz), 3.48-3.62 (2H, m),3.68-3.72 (2H, m), 4.17 (2H, q, J=8 Hz), 4.20-4.41 (2×2/3H, m), 4.65(2×1/3H, d, J=15 Hz), 4.98-5.13 (2H, m), 6.98 (2×1/3H, d, J=8 Hz), 7.08(2×2/3H, d, J=8 Hz), 7.12-7.32 (8H, m), 7.37-7.46 (2H, m), 7.70 (1×1/3H,d, J=8 Hz), 7.73 (1×2/3H, d, J=8 Hz), 7.80-7.86 (3H, m), 8.13 (1H, d,J=8 Hz)

(88) MASS (FAB) (m/z): 655 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s),2.37-2.52 (4H, m), 2.58-2.70 (1H, m), 2.59 (3×2/3H, s), 2.81 (3×1/3H,s), 2.98-3.10 (2H, m), 3.35 (1H, t, J=15 Hz), 3.43-3.58 (2H, m),3.67-3.72 (2H, m), 4.07-4.39 (2×2/3H, m), 4.63 (2×1/3H, d, J=15 Hz),5.02-5.17 (2H, m), 6.97 (2×1/3H, d, J=8 Hz), 7.07 (2×2/3H, d, J=8 Hz),7.12-7.22 (6H, m), 7.24-7.32 (3H, m), 7.63 (1H, s), 7.65-7.72 (2H, m),8.35-8.40 (1H, m), 8.62 (1H, s)

(89) MASS (FAB) (m/z): 653 (M+H)⁺ ; NMR (CDCl₃, δ): 2.29 (3H, s),2.38-2.50 (4H, m), 2.61 (3×2/3H, s), 2.58-2.70 (1H, m), 2.81 (3×1/3H,s), 2.98 (6H, s), 3.02-3.08 (2H, m), 3.25-3.35 (1H, m), 3.42-3.58 (2H,m), 3.64-3.72 (2H, m), 4.13-4.38 (2×2/3H, m), 4.65 (2×1/3H, d, J=15 Hz),5.00-5.16 (2H, m), 6.89-7.08 (5H, m), 7.13-7.22 (5H, m), 7.28-7.32 (2H,m), 7.38-7.46 (2H, m), 7.63 (1×1/3H, d, J=8 Hz), 7.70 (1×2/3H, d, J=8Hz), 8.10-8.13 (1H, m)

(90) MASS (FAB) (m/z): 702 (M+H)⁺ ; NMR (CDCl₃, δ): 2.31 (3H, s),2.38-2.50 (4H, m), 2.60-2.72 (1H, m), 2.65 (3×2/3H, s), 2.82 (3×1/3H,s), 3.00-3.12 (2H, m), 3.30-3.40 (1H, m), 3.45-3.58 (2H, m), 3.63-3.72(2H, m), 3.93 (3H, s), 4.20-4.40 (2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz),5.02-5.22 (2H, m), 7.00 (2×1/3H, d, J=8 Hz), 7.10 (2×2/3H, d, J=8 Hz),7.14-7.32 (5H, m), 7.38-7.53 (3H, m), 7.60-7.72 (2H, m), 7.90-8.00 (2H,m), 8.22-8.30 (1H, m)

(91) MASS (FAB) (m/z): 684 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28 (3H, s),2.32-2.50 (4H, m), 2.58-2.70 (1H, m), 2.66 (3×2/3H, s), 2.81 (3×1/3H,s), 2.97-3.11 (2H, m), 3.31 (1H, t, J=15 Hz), 3.44-3.58 (2H, m),3.62-3.70 (2H, m), 3.90 (3H, s), 4.23-4.41 (2×2/3H, m), 4.69 (2×1/3H, d,J=15 Hz), 5.00-5.18 (2H, m), 7.01 (2×1/3H, d, J=8 Hz), 7.09 (2×2/3H, d,J=8 Hz), 7.12-7.22 (5H, m), 7.38-7.47 (2H, m), 7.70-7.88 (4H, m), 7.92(2H, d, J=8 Hz), 8.12-8.18 (1H, m)

(92) MASS (FAB) (m/z): 667 (M+H)⁺ ; NMR (CDCl₃, δ): 2.20 (3H, s),2.27-2.42 (4H, m), 2.62 (3×2/3H, s), 2.67-2.76 (1H, m), 2.79 (3×1/3H,s), 2.93-3.10 (2H, m), 3.22 (1H, dd, J=15, 5 Hz), 3.32-3.47 (2H, m),3.52-3.70 (2H, m), 3.90 (3H, s), 4.22 (2×1/3H, d, J=15 Hz), 4.29(2×1/3H, d, J=18 Hz), 4.72 (2×1/3H, d, J=15 Hz), 5.09-5.30 (2H, m),6.92-7.03 (4H, m), 7.04-7.18 (4H, m), 7.22 (2H, t, J=8 Hz), 7.42 (1H, d,J=8 Hz), 7.66 (1H, d, J=8 Hz), 7.90 (2H, d, J=8 Hz), 8.07-8.19 (2H, m)

EXAMPLE 11

The following object compounds were obtained according to a similarmanner to that of Example 3.

(1) MASS (m/z): 667 (M+H)⁺ ; NMR (CDCl₃, δ): 2.34 (6H, s), 2.42-2.78(9H, m), 2.61 (2/3×3H, s), 2.81 (1/3×3H, s), 2.93-3.15 (2H, m),3.22-3.40 (1H, m), 3.40-3.75 (4H, m), 4.25 (1/3×2H, ABq, Δ=0.18, J=17Hz), 4.29 (2/3×1H, d, J=15 Hz), 4.65 (2/3×1H, d, J=15 Hz), 5.00-5.22(2H, m), 6.85-7.78 (16H, m), 8.15-8.25 (1H, m)

(2) MASS (m/z): 696 (M⁺ +1); NMR (CDCl₃, δ): 1.45 (9H, s), 2.62 (3H×2/3,s), 2.67 (1H, m), 2.82 (3H×1/3, s), 3.04 (2H, m), 3.28 (1H, m), 3.44(6H, m), 3.62 (2H, m), 4.14 (1H×1/3, d, J=16 Hz), 4.29 (1H×2/3, d, J=15Hz), 4.37 (1H×1/3, d, J=16 Hz), 4.63 (1H×2/3, d, J=15 Hz), 5.11 (2H, m),6.96-7.33 (11H, m), 7.44 (1H, t, J=8 Hz), 7.50 (1H, s), 7.56 (1H, d, J=8Hz), 7.67 (2H, m), 8.19 (1H, d, J=8 Hz)

(3) MASS (FAB) (m/z): 600 (M+H)⁺ ; NMR (DMSO-d₆, δ): 2.55-2.67 (2H, m),2.74 (3×1/3H, s), 2.82 (3×2/3H, s), 2.84-3.03 (2H, m), 3.42 (2H, t, J=5Hz), 3.64-3.75 (1H, m), 4.37 (2×1/3H, d, J=15 Hz), 4.53 (2×2/3H, d, J=15Hz), 4.57-4.63 (2H, m), 4.80-5.01 (2H, m), 7.03-7.10 (4H, m), 7.13-7.30(9H, m), 7.45 (1H, d, J=8 Hz), 7.63 (2H, t, J=8 Hz), 8.32 (1×2/3H, d,J=8 Hz), 8.39 (1×1/3H, d, J=8 Hz), 8.49 (1H, t, J=8 Hz)

(4) MASS (FAB) (m/z): 653 (M+H)⁺ ; NMR (CDCl₃, δ): 1.66-1.73 (2H, m),2.37-2.50 (4H, m), 2.55 (2H, t, J=5 Hz), 2.60 (3×2/3H, s), 2.59-2.72(1H, m), 2.81 (3×1/3H, s), 3.02 (2H, d, J=8 Hz), 3.18-3.27 (1H, m),3.40-3.47 (2H, m), 3.59-3.65 (2H, m), 3.76 (2H, t, J=5 Hz), 4.18-4.38(2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz), 5.11-5.22 (2H, m), 6.96-7.17(13H, m), 7.43 (1H, d, J=8 Hz), 7.63 (1H, d, J=8 Hz), 7.93-8.08 (2H, m)

(5) MASS (FAB) (m/z): 682 (M+H)⁺ ; NMR (CDCl₃, δ): 1.23 (3H, t, J=8 Hz),2.52-2.66 (4H, m), 2.58 (3×2/3H, s), 2.67 (1H, dd, J=15, 8 Hz), 2.81(3×1/3H, s), 2.97-3.11 (2H, m), 3.20 (2H, s), 3.31 (1H, t, J=15 Hz),3.47-3.62 (2H, m), 3.70-3.74 (2H, m), 4.18 (2H, q, J=8 Hz), 4.20-4.38(2×2/3H, m), 4.66 (2×1/3H, d, J=15 Hz), 5.02-5.18 (2H, m), 6.96 (2×1/3H,d, J=8 Hz), 7.06 (2×2/3H, d, J=8 Hz), 7.14-7.21 (6H, m), 7.25-7.32 (3H,m), 7.43 (1H, t, J=8 Hz), 7.50 (1H, s), 7.57 (1H, d, J=8 Hz), 7.63-7.72(2H, m), 8.18-8.22 (1H, m)

(6) MASS (FAB) (m/z): 631 (M+H)⁺ ; NMR (CDCl₃, δ): 2.68-2.80 (1H, m),2.70 (3×2/3H, s), 2.84 (3×1/3H, s), 2.90-3.08 (3H, m), 3.70-3.83 (6H,m), 4.28 (2×1/3H, d, J=15 Hz), 4.43-4.68 (2×2/3H, m), 4.54 (3H, br s),5.03-5.19 (2H, m), 7.02-7.05 (4H, m), 7.09-7.16 (4H, m), 7.23-7.33 (4H,m), 7.39 (1H, t, J=8 Hz), 7.46 (2H, t, J=8 Hz), 7.62 (1H, d, J=8 Hz),7.92 (1×1/3H, d, J=8 Hz), 8.00 (1×2/3H, d, J=8 Hz), 8.14 (1H, d, J=8 Hz)

(7) MASS (FAB) (m/z): 630 (M+H)⁺ ; NMR (CDCl₃, δ): 2.68-2.75 (1H, m),2.77 (3×2/3H, s), 2.84-3.08 (3H, m), 2.92 (3×1/3H, s), 3.65-3.77 (6H,m), 4.24-4.52 (2×2/3H, m), 4.81 (2×1/3H, d, J=15 Hz), 5.10-5.40 (2H, m),6.96-7.14 (11H, m), 7.23-7.33 (3H, m), 7.43 (1H, d, J=8 Hz), 7.64 (1H,d, J=8 Hz), 7.92 (1H, t, J=8 Hz), 8.27 (1×1/3H, d, J=8 Hz), 8.37(1×2/3H, d, J=8 Hz)

(8) MASS (FAB) (m/z): 601 (M+H)⁺ ; NMR (CDCl₃, δ): 2.67 (3×2/3H, s),2.62-2.81 (2H, m), 2.81 (3×1/3H, s), 2.88-3.07 (3H, m), 3.75-3.90 (4H,m), 3.99-4.08 (1H, m), 4.19-4.47 (2×2/3H, m), 4.21 (1H, br s), 4.33 (1H,br s), 4.70 (2×1/3H, d, J=15 Hz), 5.02-5.10 (1H, m), 5.12-5.21 (1H, m),7.00 (3H, t, J=8 Hz), 7.09-7.15 (3H, m), 7.21-7.27 (4H, m), 7.30-7.49(4H, m), 7.57 (1H, t, J=8 Hz), 8.03 (1×1/3H, d, J=8 Hz), 8.12 (1×2/3H,d, J=8 Hz), 8.21-8.23 (1H, m)

(9) MASS (ESI) (m/z): 510 (M+1); NMR (CDCl₃, δ): 1.99 (1H, dd, J=25, 8Hz), 2.61 (1H, dd, J=25, 8 Hz), 2.80-3.12 (4H, m), 2.86 (3×2/3H, s),2.92 (3×1/3H, s), 3.05 (3H, s), 3.49 (2H, d, J=8 Hz), 3.51-3.72 (1H, m),4.00 (1H, q, J=8 Hz), 4.22-4.34 (2H, m), 4.52-4.70 (3H, m), 5.20-5.28(2H, m), 6.58 (1H, d, J=8 Hz), 7.07 (2H, d, J=8 Hz), 7.16-7.32 (7H, m),7.40-7.66 (7H, m)

EXAMPLE 12

To a solution of Starting Compound (107 mg) in dichloromethane (5 ml)was added (benzo b!furan-2-yl)isocyanate (50 mg) at room temperature andstirred for 1 hour. Purification by column chromatography (silica gel,chloroform-methanol) afforded Object Compound (140 mg) as white powders.

MASS (m/z): 625 (M+H)⁺ ; NMR (CDCl₃, δ): 2.28 (3H, s), 2.30-2.48 (4H,m), 2.55 (2/3×3H, s), 2.65-2.82 (1H, m), 2.78 (1/3×3H, s), 2.95-3.15(2H, m), 3.22-3.72 (4H, m), 4.14 (2/3×1H, d, J=15 Hz), 4.22 (1/3×2H,ABq, Δ=0.16, J=17 Hz), 4.65 (2/3×1H, d, J=15 Hz), 4.78-4.95 (1H, m),5.05-5.22 (1H, m), 6.44 (1H, s), 6.82-7.82 (16H, m), 8.35-8.55 (2H, m)

EXAMPLE 13

Starting Compound (387 mg) and benzo b!furan-2-carboxaldehyde (99 mg)were dissolved in benzene (10 ml) and heated to reflux for 2 hours.After the mixture was allowed to cool to room temperature, the solventwas evaporated and the remaining solid was redissolved in methanol (1ml). To this solution was added sodium cyanoborohydride (45 mg) at roomtemperature, and added some drops of hydrogen chloride-methanol toadjust the solution to about pH 4. The reaction mixture was stirred atthe room temperature for 2 days. The mixture was evaporated, addedaqueous sodium hydrogen carbonate, and extracted three times withchloroform. The organic layer was washed with brine and dried overmagnesium sulfate. Evaporation of the solvent followed by subjecting tocolumn chromatography (silica gel, chloroform-tethanol) gave ObjectCompound (248 mg) as a viscous oil.

MASS (m/z): 596 (M+H)⁺ ; NMR (CDCl₃, δ): 2.25 (3H, s), 2.25-2.78 (7H,m), 2.68 (2/3×3H, s), 2.85 (1/3×3H, s), 2.90-3.15 (2H, m), 3.25-3.68(4H, m), 3.83 (2/3×2H, s), 3.90 (1/3×2H, ABq, Δ=0.12, J=17 Hz), 4.35(2/3×1H, d, J=15 Hz), 4.38 (1/3×2H, s), 4.70 (2/3×1H, d, J=15 Hz),5.05-5.22 (1H, m), 6.55 (1/3×1H, s), 6.60 (2/3×1H, s), 6.93-7.56 (15H,m), 8.02-8.22 (1H, m)

EXAMPLE 14

Starting Compound (53 mg) was dissolved in N,N-dimethylformamide (1 ml).Pyridinium chloride (98 mg) was added to the solution, and the mixturewas stirred at room temperature for 2.5 hours. The solvent wasevaporated, and the remaining oil was dissolved in ethyl acetate. Thesolution was washed twice with aqueous sodium hydrogen carbonate anddried over magnesium sulfate. Evaporation of the solvent followed bysubjecting to column chromatography (silica gel, chloroform-methanol)afforded Object Compound (24 mg) as white powder.

MASS (m/z): 586 (M+H)⁺ ; NMR (CDCl₃, δ): 2.58-3.20 (3H, m), 2.88(1/3×3H, s), 3.01 (2/3×3H, s), 3.28-3.80 (9H, m), 4.27 (2/3×1H, d, J=15Hz), 4.62 (1/3×2H, ABq, Δ=0.09, J=17 Hz), 4.80 (2/3×1H, d, J=15 Hz),4.98-5.35 (2H, m), 6.45-8.22 (15H, m), 8.65 (1H, br s)

EXAMPLE 15

Starting Compound (347 mg) was dissolved in a mixture of 15% aqueoussodium hydroxide (1 ml) and ethanol (2 ml), and the solution was stirredat room temperature for 1 hour. The solution was acidified by adding 6Nhydrochloric acid and extracted three times with chloroform. The organiclayer was dried over sodium sulfate. Purification by columnchromatography (silica gel, chloroform-methanol) gave Object Compound(151 mg) as white powder.

MASS (m/z): 640 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.70 (1H, m), 2.73(2/3×3H, s), 2.88 (1/3×3H, s), 2.92-3.75 (11H, m), 4.22 (1/3×1H, d, J=17Hz), 4.28 (2/3×1H, d, J=15 Hz), 4.55 (1/3×1H, d, J=17 Hz), 4.62 (2/3×1H,d, J=15 Hz), 5.02-5.35 (2H, m), 6.75-8.45 (17H, m)

EXAMPLE 16

Starting Compound (155 mg), N-(2-chloroethyl)-dimethylaminehydrochloride (62 mg), and potassium carbonate were mixed inN,N-dimethylformamide (0.5 ml) and heated to 50° C. for 8 hours. Thereaction mixture was diluted with ethyl acetate, washed twice withaqueous sodium hydrogencarbonate, twice with aqueous sodium hydroxide,once with brine, and dried over magnesium sulfate. Purification bycolumn chromatography (chloroform-methanol) gave Object Compound (32 mg)as white powder.

MASS (m/z): 684 (M+H)⁺ ; NMR (CDCl₃, δ): 2.34 (6H, s), 2.58 (2/3×3H, s),2.58-2.80 (3H, m), 2.78 (1/3×3H, s), 2.95-3.12 (2H, m), 3.23-3.39 (1H,m), 3.39-3.80 (8H, m), 4.00-4.10 (2H, m), 4.02 (1/3×1H, d, J=17 Hz),4.22 (2/3×1H, d, J=15 Hz), 4.31 (1/3×1H, d, J=17 Hz), 4.59 (2/3×1H, d,J=15 Hz), 5.02-5.20 (2H, m), 6.68-7.75 (15H, m), 8.15-8.26 (1H, m)

EXAMPLE 17

To a solution of Starting Compound (92 mg) in dichloromethane (0.5 ml)was added iodomethane (100 mg) at room temperature and stirred for 12hours. Ether was added to the mixture and pale-yellow precipitate formedwas removed by filtration and dried in vacuo to give Object Compound(103 mg).

MASS (m/z): 624 (M-I)⁺ ; NMR (CDCl₃, δ): 2.70-2.88 (1H, m), 2.83 (3H,s), 2.90-3.25 (3H, m), 3.25-4.18 (14H, m), 4.45 (2/3×2H, ABq, Δ=0.05,J=15 Hz), 4.47 (1/3×2H, ABq, Δ=0.18, J=17 Hz), 4.98-5.25 (2H, m),7.00-8.05 (17H, m)

EXAMPLE 18

The following object compounds were obtained according to a similarmanner to that of Preparation 10.

(1) MASS (FAB) (m/z): 613 (M+H)⁺ ; NMR (CDCl₃ -DMSO-d₆, δ): 2.57-2.70(1H, m), 2.72 (3×1/3H, s) 2.82 (3×2/3H, s), 2.83-3.05 (3H, m), 3.38-3.45(4H, m), 3.49-3.53 (2H, m), 3.57-3.60 (2H, m), 4.38-4.52 (2H, m),4.82-5.02 (2H, m), 5.29 (2H, s), 7.02-7.32 (11H, m), 7.38 (1H, s), 7.85(1H, s), 8.27-8.37 (1H, m), 8.56-8.64 (1H, m)

(2) MASS (FAB) (m/z): 625 (M+H)⁺ ; NMR (CDCl₃, δ): 2.29 (3H, s),2.33-2.49 (4H, m), 2.58-2.70 (1H, m), 2.63 (3×2/3H, s), 2.81 (3×1/3H,s), 2.97-3.11 (2H, m), 3.25-3.35 (1H, m), 3.42-3.54 (2H, m), 3.61-3.70(2H, m), 4.08-4.38 (2×2/3H, m), 4.63 (2×1/3H, d, J=15 Hz), 5.01-5.18(2H, m), 6.81 (1H, dd, J=8, 2 Hz), 6.87 (1H, d, J=2 Hz), 6.95 (2×1/3H,d, J=8 Hz), 7.06 (2×2/3H, d, J=8 Hz), 7.12-7.22 (5H, m), 7.22-7.28 (3H,m), 7.30-7.33 (2H, m), 7.62-7.75 (1H, m), 8.10-8.15 (1H, m)

EXAMPLE 19

To an ethanol (5 ml) solution of Starting Compound (488 mg) was addedethanol (5 ml) solution of citric acid (169 mg) at room temperature. Themixture was concentrated to about 2 ml, and diluted with 300 ml ofwater. The water was removed by freeze dryer to give Object Compound(569 mg) as white powders.

NMR (D₂ O, δ): 2.65 (4H, ABq, Δ=0.12, J=16 Hz), 2.5-3.5 (18H, m),3.8-5.0 (4H, m), 6.8-7.7 (17H, m)

EXAMPLE 20

The following object compounds were obtained according to a similarmanner to that of Example 19.

(1) NMR (D₂ O, δ): 2.65 (6H, ABq, Δ=0.12, J=16 Hz), 2.5-3.5 (18H, m),3.8-4.9 (4H, m), 6.6-7.6 (17H, m) (2) NMR (D₂ O, δ): 2.73 (8H, ABq,Δ=0.12, J=16 Hz), 2.4-3.6 (18H, m), 3.8-5.0 (4H, m), 6.5-7.5 (17H, m)

(3) MASS (FAB) (m/z): 668; NMR (CD₃ OD, δ): 2.72-2.78 (5H, m), 2.83-2.87(5H, m), 2.89-3.10 (6H, m), 3.12-3.18 (2H, m), 3.77-3.85 (3H, m), 3.89(3H, s), 4.48 (2×1/2H, d, J=15 Hz), 4.63 (2×1/2H, d, J=15 Hz), 4.98-5.15(3H, m), 7.12-7.24 (7H, m), 7.33 (1H, t, J=8 Hz), 7.48 (1H, t, J=8 Hz),7.52 (1H, s), 7.60 (1H, d, J=8 Hz), 7.73 (1H, d, J=8 Hz), 7.92 (2H, d,J=8 Hz)

EXAMPLE 21

The following object compound was obtained according to a similar mannerto that of Preparation 3, 4 or 8.

MASS (m/z): 596 (M⁺ +1); NMR (CDCl₃, δ): 2.61 (3H×2/3, s), 2.67 (1H, m),2.81 (3H×1/3, s), 2.86 (4H, m), 3.05 (2H, m), 3.31 (1H, m), 3.44 (2H,m), 3.63 (2H, m), 4.15 (1H×1/3, d, J=16 Hz), 4.29 (1H×2/3, d, J=15 Hz),4.35 (1H×1/3, d, J=16 Hz), 4.64 (1H×2/3, d, J=15 Hz), 5.10 (2H, m), 6.96(2H×1/3, m), 7.05 (2H×2/3, m), 7.17 (5H, s), 7.25-7.33 (5H, m), 7.43(1H, t, J=8 Hz), 7.50 (1H, s), 7.57 (1H, d, J=8 Hz), 7.66-7.74 (2H, m),8.22 (1H, m)

EXAMPLE 22

To a solution of Starting Compound (1.0 g) in methanol (10 ml) was addeddropwise 10% hydrochloric acid-methanol solution (1 ml). Evaporation ofsolvent gave Object Compound (1.06 g).

NMR (CDCl₃, δ): 2.56 (3H×2/3, s), 2.70 (3H×1/3, s), 2.78 (2H, m), 2.86(3H×1/3, s), 2.93 (3H×2/3, s), 3.00-3.24 (4H, m), 3.35-3.57 (3H, m),3.65-3.91 (1H, m), 4.02-4.05 (1H, m), 4.38 (1H, d, J=15 Hz), 4.55 (1H,d, J=15 Hz), 4.63-4.75 (1H, m), 5.06 (1H, m), 5.06 (1H×1/3, m), 5.28(1H×2/3, m), 7.05-7.33 (11H, m), 7.40-7.58 (4H, m), 7.67 (1H, d, J=8Hz), 7.76 (1H, t, J=4 Hz)

EXAMPLE 23

The following object compound was obtained according to a similar mannerto that of Preparation 10.

MASS (FAB) (m/z): 629 (M+H)⁻ ; NMR (CDCl₃, δ): 2.59-2.70 (1H, m), 2.67(3×2/3H, s), 2.81 (3×1/3H, s), 3.04-3.14 (2H, m), 3.39 (1H, dd, J=15, 5Hz), 3.44-3.51 (2H, m), 3.60-3.78 (6H, m), 4.11-4.42 (2×2/3H, m), 4.68(2×1/3H, d, J=15 Hz), 5.08-5.15 (1H, m), 5.23-5.32 (1H, m), 6.93-7.03(2H, m), 7.18-7.36 (9H, m), 7.51 (1H, d, J=8 Hz), 7.71 (1H, t, J=8 Hz),7.95 (1H, s), 8.22 (1H, d, J=8 Hz)

EXAMPLE 24

The crude Object compound was obtained according to a similar manner tothat of Example 1. About 30 g of the product was obtained, and it wasrecrystallized from ethanol-water (2:1) to give 28.47 g of whitecrystals.

mp: 92-93° C.; MASS: m/z 562 (M+H)⁺ ; NMR (CDCl₃, δ): 2.59 (4/5×3H, s),2.77 (1/5×3H, s), 2.91 (2H, d, J=7 Hz), 3.32 (1H, dd, J=14 and 7 Hz),3.47 (1H, dd, J=14 and 4 Hz), 4.11 (1/5×1H, d, J=16 Hz), 4.27 (4/5×1H,d, J=15 Hz), 4.29 (1/5×1H, d, J=16 Hz), 4.60 (4/5×1H, d, J=15 Hz),5.02-5.13 (2H, m), 7.08-7.37 (10H, m), 7.43 (1H, t, J=8 Hz), 7.48 (1H,s), 7.55-7.69 (3H, m), 8.18 (1H, m), 8.26 (1/5×1H, d, J=2 Hz), 8.37(4/5×1H, d, J=2 Hz), 8.51 (1H, d, J=4 Hz), 8.58 (1H, d, J=4 Hz), 8.65(1H, d, J=7 Hz)

EXAMPLE 25

Object compounds were obtained according to a similar manner to that ofExample 1 or 24.

(1) MASS: m/z 578 (M⁺ +1); NMR (CDCl₃, δ): 2.60 (3H×3/4, s), 2.76(3H×1/4, s), 2.87 (2H, d, J=7 Hz), 3.27 (1H, m), 3.42 (1H, m), 4.12(1H×1/4, d, J=16 Hz), 4.29 (1H×3/4, d, J=15 Hz), 4.32 (1H×1/4, d, J=16Hz), 4.58 (1H×3/4, d, J=15 Hz), 4.97-5.13 (2H, m), 7.09-7.29 (8H, m),7.35-7.45 (3H, m), 7.63 (1H, t, J=8 Hz), 7.85-7.88 (3H, m), 8.10(1H×3/4, d, J=8 Hz), 8.22 (1H×1/4, d, J=8 Hz), 8.37 (1H, s), 8.51 (1H,m), 8.57 (1H, m), 8.69 (1H, d, J=8 Hz)

(2) MASS: m/z 561 (M⁺ +1); NMR (CDCl₃, δ): 2.64 (3H×3/4, s), 2.81(3H×1/4, s), 2.82-3.05 (2H, m), 3.37 (2H, m), 4.17 (1H×1/4, d, J=16 Hz),4.24 (1H×1/4, d, J=16 Hz), 4.36 (1H×3/4, d, J=15 Hz), 4.58 (1H×3/4, d,J=15 Hz), 5.17 (1H, q, J=7 Hz), 5.35 (1H×3/4, q, J=7 Hz), 5.44 (1H×1/4,q, J=7 Hz), 7.03-7.32 (12H, m), 7.38-7.49 (2H, m), 7.67 (1H, d, J=8 Hz),8.22-8.71 (5H, m)

(3) MASS: m/z 599 (M⁺ +1); NMR (CDCl₃, δ): 2.51 (3H×2/3, s), 2.78(3H×1/3, s), 2.89 (2H, m), 3.26 (1H, m), 3.43 (1H×2/3, m), 3.47 (1H×1/3,m), 4.17 (2H×1/3, s), 4.21 (1H×2/3, d, J=15 Hz), 4.56 (1H×2/3, d, J=15Hz), 4.96-5.08 (2H, m), 6.81 (1H, d, J=8 Hz), 6.92 (1H, m), 6.99-7.12(8H, m), 7.16 (1H, t, J=8 Hz), 7.24-7.32 (5H, m), 7.35-7.50 (4H, m),7.64 (1H, d, J=8 Hz), 7.73 (1H, m), 8.25 (1H×2/3, br s), 8.35 (1H×1/3,br s)

(4) MASS: m/z 598 (M⁺ +1); NMR (CDCl₃, δ): 2.46(3H×2/3, s), 2.80(3H×1/3, s), 2.88-3.02 (2H, m), 3.21-3.37 (2H, m), 3.75 (1H×1/3, d, J=16Hz), 4.15 (1H×2/3, d, J=15 Hz), 4.19 (1H×1/3, d, J=16 Hz), 4.77 (1H×2/3,d, J=15 Hz), 5.19 (1H, m), 5.62-5.73 (1H, m), 6.76 (1H, m), 6.90-7.26(18H, m), 7.47 (1H, d, J=8 Hz), 7.55-7.67 (3H, m), 8.92 (1H, d, J=8 Hz)

(5) MASS: m/z 550 (M⁺ +1); NMR (CDCl₃, δ): 2.65 (3H×2/3, s), 2.85(3H×1/3, s), 2.93-3.02 (2H, m), 3.12-3.31 (2H, m), 4.22 (1H×1/3, d, J=16Hz), 4.39 (1H×1/3, d, J=16 Hz), 4.44 (1H×2/3, d, J=15 Hz), 4.58 (1H×2/3,d, J=15 Hz), 4.95-5.13 (2H, m), 6.81 (1H, s), 7.01-7.08 (3H, m), 7.13(4H, s), 7.24-7.28 (5H, m), 7.38 (1H, t, J=8 Hz), 7.45-7.52 (3H, m),7.62 (1H, br s), 7.96 (1H, br s), 8.20 (1H×1/3, d, J=8 Hz), 8.30(1H×2/3, d, J=8 Hz)

(6) MASS: m/z 549 (M⁺ +1); NMR (CDCl₃, δ): 2.67 (3H×2/3, s), 2.91(3H×1/3, s), 2.93-3.03 (2H, m), 3.16 (2H, m), 4.30 (1H×2/3, d, J=15 Hz),4.31 (2H×1/3, s), 4.80 (1H×2/3, d, J=15 Hz), 5.26 (1H, m), 5.53 (1H, m),6.65 (1H, s), 6.90-7.10 (10H, m), 7.19-7.27 (6H, m), 7.45 (1H, d, J=8Hz), 7.62 (1H, d, J=8 Hz), 7.67 (1H, m), 8.95 (1H, br s)

(7) MASS: m/z 561 (M⁺ +1); NMR (CDCl₃, δ): 2.57 (3H×2/3, s), 2.80(3H×1/3, s), 2.87-2.98 (2H, m), 3.23-3.49 (2H, m), 4.15 (1H×1/3, d, J=16Hz), 4.28 (1H×2/3, d, J=15 Hz), 4.31 (1H×1/3, d, J=16 Hz), 4.60 (1H×2/3,d, J=15 Hz), 5.03-5.20 (2H, m), 6.92-7.31 (13H, m), 7.38-7.67 (5H, m),8.17 (1H×2/3, d, J=8 Hz), 8.33 (1H×1/3, d, J=8 Hz), 8.52-8.62 (2H, m)

(8) MASS: m/z 595 (M⁺); NMR (CDCl₃, δ): 2.64 (3H×5/6, s), 2.75 (3H×1/6,s), 2.79-2.97 (2H, m), 3.34 (2H, m), 4.11 (1H×1/6, d, J=16 Hz), 4.24(1H×1/6, d, J=16 Hz), 4.34 (1H×5/6, d, J=15 Hz), 4.47 (1H×5/6, d, J=15Hz), 5.10-5.23 (2H, m), 7.02-7.28 (12H, m), 7.44 (1H, dd, J=8, 10 Hz),7.53 (1H, t, J=8 Hz), 7.68 (1H, d, J=8 Hz), 8.08-8.33 (2H, m), 8.52 (2H,m)

(9) MASS: m/z 612 (M⁺); NMR (CDCl₃, δ): 2.62 (3H×4/5, s), 2.74 (3H×1/5,s), 2.87 (2H, d, J=7nz), 3.29 (1H, m), 3.43 (1H, m), 4.10 (1H×1/5, d,J=16 Hz), 4.22 (1H×1/5, d, J=16 Hz), 4.27 (1H×4/5, d, J=15 Hz), 4.52(1H×4/5, d, J=15 Hz), 5.01 (1H, m), 5.08 (1H, m), 7.05-7.33 (9H, m),7.38-7.47 (2H, m), 7.63 (1H, m), 7.87-7.90 (3H, m), 8.07-8.24 (2H, m),8.57 (1H, m), 8.67 (1H×1/5, d, J=8 Hz), 8.73 (1H×4/5, d, J=8 Hz)

(10) MASS: m/z 596 (M⁺); NMR (CDCl₃, δ): 2.62 (3H×5/6, s), 2.74 (3H×1/6,s), 2.91 (2H, d, J=7 Hz), 3.32 (1H, m), 3.45 (1H, m), 4.12 (1H×1/6, d,J=16 Hz), 4.22 (1H×1/6, d, J=16 Hz), 4.25 (1H×5/6, d, J=15 Hz), 4.52(1H×5/6, d, J=15 Hz), 5.04-5.15 (2H, m), 7.08-7.32 (10H, m), 7.44 (1H,m), 7.49 (1H, s), 7.55 (1H, t, J=8 Hz), 7.62-7.69 (2H, m), 8.03 (1H×1/6,m), 8.14 (1H×5/6, m), 8.22 (1H, d, J=8 Hz), 8.58-8.68 (2H, m)

(11) MASS: m/z 578 (M⁺ +1); NMR (CDCl₃, δ): 2.17 (3H×3/4, s), 2.82(3H×1/4, s), 2.91-3.02 (2H, m), 3.20-3.47 (2H, m), 4.16-4.55 (2H, m),4.93-5.22 (2H, m), 6.73-6.87 (2H, m), 7.05-7.22 (6H, m), 7.37-7.45 (2H,m), 7.59-7.65 (1H, m), 7.84-7.88 (3H, m), 8.05-8.25 (1H, m), 8.33-8.71(4H, m)

(12) MASS: m/z 579 (M⁺ +1); NMR (CDCl₃, δ): 2.67 (3H×2/3, s), 2.81(3H×1/3, s), 2.88-3.06, (2H, m), 3.17-3.52 (2H, m), 4.21 (1H×1/4, d,J=15 Hz), 4.37 (1H×1/4, d, J=15 Hz), 4.35 (1H×3/4, d, J=15 Hz), 4.52(1H×3/4, d, J=15 Hz), 4.96-5.27 (2H, m), 6.74-6.88 (2H, m), 7.03-7.25(6H, m), 7.46-7.64 (3H, m), 7.95 (1H, m), 8.11-9.20 (5H, m)

(13) MASS: 562 (M⁺ +1); NMR (CDCl₃, δ): 2.68 (3H×3/4, s), 2.81 (3H×1/4,s), 2.88-3.05 (2H, m), 3.13-3.48 (2H, m), 4.22 (1H×1/4, d, J=15 Hz),4.34 (1H×3/4, d, J=15 Hz), 4.35 (1H×1/4, d, J=15 Hz), 4.53 (1H×3/4, d,J=15 Hz), 4.94-5.25 (2H, m), 6.73-6.76 (2H×1/4, m), 6.86-6.88 (2H×3/4,m), 7.03-7.22 (6H, m), 7.26-7.32 (2H, m), 7.40-7.68 (5H, m), 8.15-8.65(5H, m)

(14) MASS m/z 561 (M⁺ +1); NMR (CDCl₃, δ): 2.67 (3H×3/4, s), 2.83(3H×1/4, s), 2.77-3.06 (2H, m), 3.22-3.44 (2H, m), 4.13 (1H×1/4, d, J=15Hz), 4.25 (1H×3/4, d, J=15 Hz), 4.42 (1H×1/4, d, J=15 Hz), 4.63 (1H×3/4,d, J=15 Hz), 4.98-5.40 (2H, m), 6.68-6.72 (2H×1/4, m), 6.82-6.84(2H×3/4, m), 6.97-7.23 (10H, m), 7.37-7.53 (2H, m), 7.66-7.69 (1H, m),8.24-8.62 (5H, m)

(15) MASS: m/z 560 (M⁺ +1); NMR (CDCl₃, δ): 2.63 (3H×3/4, s), 2.87(3H×1/4, s), 2.90-3.01 (2H, m), 3.32-3.37 (2H, m), 4.17 (1H×1/4, d, J=15Hz), 4.28 (1H×3/4, d, J=15 Hz), 4.72 (1H×1/4, d, J=15 Hz), 4.74 (1H×3/4,d, J=15 Hz), 5.21 (111, m), 5.46 (1H, m), 6.88-7.24 (15H, m), 7.37-7.48(2H, m), 7.17-8.25 (1H, m), 8.40-8.61 (2H, m)

EXAMPLE 26

The following object compounds were obtained according to a similarmanner to that of Example 1 or 24.

(1) MASS: 530 (M+1); NMR (CDCl₃, δ): 2.15 (3×1/3H, s), 2.17 (3×2/3H, s),2.67 (3×2/3H, s), 2.91 (3×1/3H, s), 2.82-3.13 (4H, m), 4.12 (2×1/6H, d,J=16 Hz), 4.39 (2×1/6H, d, J=16 Hz), 4.41 (2×1/3H, d, J=15 Hz), 4.63(2×1/3H, d, J=15 Hz), 4.78-4.88 (1H, m), 5.17-5.23 (1H, m), 6.99-7.57(16H, m), 7.70 (1H, d, J=8 Hz)

(2) MASS: 529 (M+1); NMR (CDCl₃, δ): 2.17 (3H, s), 2.72 (3×2/3H, s),2.98 (3×1/3H, s), 2.95-3.10 (4H, m), 4.19 (2×1/6H, d, J=16 Hz), 4.39(2×1/6H, d, J=16 Hz), 4.52 (2×1/3H, d, J=15 Hz), 4.80 (2×1/3H, d, J=15Hz), 5.38-5.49 (1H, m), 5.60-5.70 (1H, m), 6.97-7.18 (9H, m), 7.21-7.33(5H, m), 7.51 (1H, d, J=8 Hz), 7.68 (1H, d, J=8 Hz ), 9.10 (1×1/3H, d,J=8 Hz), 9.15 (1×2/3H, d, J=8 Hz)

(3) MASS: 535 (M+1); NMR (CDCl₃, δ): 2.73 (3×2/3H, s), 2.80 (3×1/3H, s),2.99-3.16 (2H, m), 3.72-3.82 (1H, m), 4.07-4.23 (2H, m), 4.42 (2×1/2H,d, J=15 Hz), 4.53 (2×1/2H, d, J=15 Hz), 4.82-4.90 (1H, m), 5.11-5.20(1H, m), 7.09-7.31 (7H, m), 7.32-7.45 (2H, m), 7.50 (1H, d, J=8 Hz),7.51 (1H, m), 7.57 (1H, t, J=8 Hz), 7.63 (1H, d, J=8 Hz), 7.79 (1H, d,J=8 Hz), 8.15 (1×1/3H, s), 8.20 (1×2/3H, s)

(4) MASS: 551 (M+1); NMR (CDCl₃, δ): 2.69 (3×2/3H, s), 2.78 (3×1/3H, s),2.98-3.14 (2H, m), 3.73-3.82 (1H, m), 4.06-4.14 (1H, m), 4.18 (1H, t,J=8 Hz), 4.00 (2×1/6H, d, J=16 Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.38(2×1/3H, d, J=15 Hz), 4.51 (2×1/3H, d, J=15 Hz), 4.80-4.87 (1H, m),5.09-5.18 (1H, m), 7.07-7.30 (6H, m), 7.31-7.43 (4H, m), 7.73-7.87 (4H,m), 8.12 (1×1/3H, s), 8.17 (1×2/3H, s)

(5) MASS: 534 (M+1); NMR (CDCl₃, δ): 2.91 (3×1/4H, s), 2.93 (3×3/4H, s),3.01-3.25 (2H, m), 3.91-4.08 (2H, m), 4.09 (2×1/8H, d, J=16 Hz), 4.30(2×1/8H, d, J=16 Hz), 4.35 (2×3/8H, d, J=15 Hz), 4.65 (2×3/8H, d, J=15Hz), 5.20-5.38 (2H, m), 5.40-5.50 (1×1/4H, m), 5.57-5.73 (1×3/4H, m),6.81 (1H, d, J=8 Hz), 7.00 (1H, s), 7.09-7.31 (9H, m), 7.42 (1H, d, J=8Hz), 7.68 (1H, d, J=8 Hz), 8.08 (1×1/4H, s), 8.13 (1×3/4H, s), 9.19 (1H,d, J=8 Hz)

(6) MASS: 758 (M+1); NMR (CDCl₃, δ): 2.61 (3×2/3H, s), 2.62-2.68 (1H,m), 2.80 (3×1/3H, s), 2.82-2.91 (1H, m), 2.93-3.04 (2H, m), 4.20-4.30(1H, m), 4.12 (2×1/4H, d, J=16 Hz), 4.22 (2×1/4H, d, J=16 Hz), 4.31(2×1/4H, d, J=15 Hz), 4.60 (2×1/4H, d, J=15 Hz), 5.11 (1H, q, J=15 Hz),6.69-7.71 (32H, m)

(7) MASS: 774 (M+1); NMR (CDCl₃, δ): 2.58-2.63 (1H, m), 2.61 (3×2/3H,s), 2.77 (3×1/3H, s), 2.81-3.06 (3H, m), 4.10-4.32 (1H, m), 4.10(2×1/4H, d, J=16 Hz), 4.22 (2×1/4H, d, J=16 Hz), 4.30 (2×1/4H, d, J=15Hz), 4.59 (2×1/4H, d, J=15 Hz), 5.10 (1H, q, J=8 Hz), 6.59 (1H, t, J=8Hz), 6.78 (1×1/3H, d, J=8 Hz), 6.86 (1×2/3H, d, J=8 Hz), 6.90-7.20 (19H,m), 7.39-7.46 (8H, m), 7.68 (1H, d, J=8 Hz), 7.83 (2H, t, J=8 Hz)

(8) MASS: 757 (M+1); NMR (CDCl₃, δ): 2.51-2.69 (2H, m), 2.72 (3×2/3H,s), 2.90-3.06 (2H, m), 2.98 (3×1/3H, s), 4.25 (2×1/3H, s), 4.39 (2×1/3H,d, J=15 Hz), 4.88 (2×1/3H, d, J=15 Hz), 5.22-5.37 (2H, m), 6.78 (1H, d,J=8 Hz), 6.87-6.93 (2H, m), 6.98-7.20 (18H, m), 7.20-7.40 (8H, m), 7.51(1H, d, J=8 Hz), 7.70 (1H, d, J=8 Hz), 8.63 (1H, t, J=8 Hz)

(9) MASS: 551 (M+1); NMR (CDCl₃, δ): 2.82 (3×2/3H, s), 2.91 (3×1/3H, s),3.01-3.20 (2H, m), 3.73-3.87 (1H, m), 4.07-4.19 (1H, m), 4.32 (2×1/6H,d, J=16 Hz), 4.63 (2×1/6H, d, J=16 Hz), 4.67 (2×1/3H, d, J=15 Hz), 4.71(2×1/3H, d, J=15 Hz), 4.61 (1H, br s), 4.85-4.98 (1H, m), 5.17-5.33 (1H,m), 7.03-7.20 (5H, m), 7.27 (1H, t, J=8 Hz), 7.36-7.80 (8H, m),7.83-7.94 (2H, m), 8.08 (1×2/3H, d, J=8 Hz), 8.10 (1×1/3H, d, J=8 Hz),8.77 (1H, s)

(10) MASS: 550 (M+1); NMR (CDCl₃, δ): 3.00 (3H, s), 3.04-3.20 (1H, m),3.20-3.32 (1H, m), 3.93-4.15 (2H, m), 4.22 (2×1/6H, d, J=16 Hz), 4.52(2×1/3H, d, J=15 Hz), 4.60 (2×1/6H, d, J=16 Hz), 4.92 (2×1/3H, d, J=15Hz), 5.30-5.50 (1H, m), 5.58-5.77 (1H, m), 6.58 (1×1/4H, s), 6.73(1×3/4H, s), 7.00-7.32 (8H, m), 7.33-7.49 (6H, m), 7.96 (1H, d, J=8 Hz),8.64 (1H, s), 9.23 (1H, d, J=8 Hz)

(11) MASS (m/z): 590 (M+1); NMR (CDCl₃, δ): 2.90 (3H×1/4, s), 3.03(3H×3/4, s), 3.14 (1H, m), 3.28 (1H, m), 3.70 (1H, m), 3.92 (1H, m),4.21-4.69 (4H, m), 4.90 (1H, m), 5.22 (1H, m), 5.54 (1H, m), 6.92-7.27(14H, m), 7.33-7.42 (2H, m), 7.66 (1H, d, J=8 Hz), 8.32-8.38 (2H, m)

(12) MASS (m/z): 589 (M⁺ +1); NMR (CDCl₃, δ): 2.68 (3H×2/3, s), 2.90(3H×1/3, s), 3.05 (2H, m), 3.77 (1H, m), 3.92 (1H, m), 4.14 (1H×1/3, d,J=15 Hz), 4.28 (1H×2/3, d, J=15 Hz), 4.38 (1H×1/3, d, J=15 Hz), 4.47(1H, d, J=15 Hz), 4.54 (1H, d, J=15 Hz), 4.81 (1H×2/3, d, J=15 Hz), 5.34(1H, q, J=7 Hz), 5.47 (1H, m), 6.92 (1H, m), 7.00 (1H, d, J=2 Hz),7.08-7.33 (17H, m), 7.47 (1H, d, J=8 Hz), 7.68 (1H, d, J=8 Hz), 8.64(1H, d, J=8 Hz)

(13) MASS (m/z): 500 (M⁺ +1); NMR (CDCl₃ 6): 2.94 (3H×3/4, s), 2.95(3H×1/4, s), 3.11 (1H, dd, J=5, 12 Hz), 3.24 (1H, dd, J=7, 12 Hz), 3.98(2H, m), 4.38 (1H×1/4, d, J=15 Hz), 4.39 (1H×3/4, d, J=15 Hz), 4.48(1H×1/4, d, J=15 Hz), 4.79 (1H×3/4, d, J=15 Hz), 5.33 (1H, m), 5.57 (1H,m), 6.96 (2H, m), 7.08-7.32 (9H, m), 7.47 (1H, d, J=8 Hz), 7.65 (1H, d,J=8 Hz), 8.32 (1H, dd, J=2, 6 Hz), 8.36 (1H, d, J=2 Hz), 9.05 (1H×1/4,d, J=8 Hz), 9.12 (1H×3/4, d, J=8 Hz)

(14) MASS: 501 (M⁺ +1); NMR (CDCl₃, δ): 2.77 (3H×3/4, s), 2.85 (3H×1/4,s), 3.06 (2H, m), 3.77 (1H, dd, J=7, 12 Hz), 4.12 (1H, m), 4.25 (1H×1/4,d, J=15 Hz), 4.48 (1H×1/4, d, J=15 Hz), 4.47 (1H×3/4, d, J=15 Hz), 4.57(1H×3/4, d, J=15 Hz), 4.83 (1H, m), 5.16 (1H, q, J=7 Hz), 7.14 (4H, s),7.18-7.72 (10H, m), 8.39 (1H×1/4, d, J=2 Hz), 8.42 (1H×3/4, d, J=2 Hz),8.51 (1H, m)

(15) MASS (m/z): 517 (M⁺ +1); NMR (CDCl₃, δ): 2.77 (3H×3/4, s), 2.87(3H×1/4, s), 3.04 (2H, m), 3.72 (1H, m), 3.89 (1H, m), 4.13 (1H, m),4.48 (1H×3/4, d, J=15 Hz), 4.49 (1H×1/4, d, J=15 Hz), 4.52 (1H×1/4, d,J=15 Hz), 4.58 (1H×3/4, d, J=15 Hz), 4.72 (1H, m), 5.12 (1H, q, J=7 Hz),7.11-7.51 (11H, m), 7.80-7.87 (3H, m), 8.42 (1H×1/4, d, J=2 Hz), 8.45(1H×3/4, d, J=2 Hz), 8.53 (1H, m)

(16) MASS (m/z): 518 (M⁺ +1); NMR (CDCl₃, δ): 2.80 (3H×4/5, s), 2.88(3H×1/5, s), 2.97-3.15 (2H, m), 3.80 (1H, t, J=7 Hz), 4.08-4.20 (2H, m),4.34 (1H×1/5, d, J=15 Hz), 4.41 (1H×1/5, d, J=15 Hz), 4.46 (1H×4/5, d,J=15 Hz), 4.55 (1H×4/5, d, J=15 Hz), 4.71-4.82 (1H, m), 5.07 (1H×1/5, q,J=7 Hz), 5.22 (1H×4/5, q, J=7 Hz), 6.64-6.97 (2H, m), 7.08-7.21 (5H, m),7.46-7.62 (3H, m), 7.95 (1H, d, J=8 Hz), 8.07 (1H, d, J=8 Hz), 8.04-8.32(1H, m), 8.49-8.52 (2H, m)

(17) MASS (m/z): 517 (M⁺ +1); NMR (CDCl₃, δ): 2.77 (3H×3/4, s), 2.85(3H×1/4, s), 2.95-3.14 (2H, m), 3.72-3.81 (1H, m), 4.08 (1H, dt, J=4, 12Hz), 4.27 (1H×1/4, d, J=15 Hz), 4.37 (1H×1/4, d, J=15 Hz), 4.42 (1H×3/4,d, J=15 Hz), 4.53 (1H×3/4, d, J=15 Hz), 4.73-4.85 (1H, m), 5.05 (1H×1/4,q, J=7 Hz), 5.18. (1H×3/4, q, J=7 Hz), 6.90-6.93 (2H, m), 7.07-7.21 (5H,m), 7.33-7.42 (3H, m), 7.77-7.87 (4H, m), 8.46-8.50 (2H, m)

(18) MASS (m/z): 500 (M⁺ +1); NMR (CDCl₃, δ): 2.73 (3H×3/4, s), 2.89(3H×1/4, s), 2.97-3.17 (2H, m), 3.83-4.02 (2H, m), 4.10 (1H×1/4, d, J=15Hz), 4.20 (1H×1/4, d, J=15 Hz), 4.37 (1H×3/4, d, J=15 Hz), 4.57 (1H×3/4,d, J=15 Hz), 5.10-5.18 (1H×1/4, m), 5.35-5.42 (1H×3/4, m), 5.50-5.57(1H, m), 6.71 (2H×1/4, d, J=7 Hz), 6.83 (2H×3/4, d, J=7 Hz), 7.06-7.23(8H, m), 7.37 (1H, d, J=8 Hz), 7.56 (1H, d, J=8 Hz), 7.63 (1H, d, J=8Hz), 8.37-8.40 (2H, m), 8.97-9.02 (1H, m)

(19) MASS (m/z): 501 (M⁺ +1); NMR (CDCl₃, δ): 2.80 (3H×3/4, s), 2.88(3H×1/4, s), 2.95-3.15 (2H, m), 3.71-3.78 (1H, m), 4.11 (1H, dt, J=4, 12Hz), 4.35 (1H×1/4, d, J=15 Hz), 4.40 (1H×1/4, d, J=15 Hz), 4.46 (1H×3/4,d, J=15 Hz), 4.56 (1H×3/4, d, J=15 Hz), 4.72-4.85 (1H, m), 5.06 (1H×1/4,q, J=7 Hz), 5.21 (1H×3/4, q, J=7 Hz), 6.92-6.97 (2H, m), 7.07-7.21 (5H,m), 7.28-7.78 (7H, m), 8.50-8.53 (2H, m)

(20) MASS (m/z): 525 (M⁺ +1); NMR (CDCl₃, δ): 0.96 (6H, d, J=6 Hz),1.54-1.80 (3H, m), 2.70 (3H×1/3, s), 2.79 (3H×2/3, s), 2.95-3.11 (2H,m), 4.47 (1H×1/3, d, J=15 Hz), 4.55 (1H×2/3, d, J=15 Hz), 4.63 (1H×1/3,d, J=15 Hz), 4.73 (1H×2/3, d, J=15 Hz), 5.42 (2H, m), 6.92-7.15 (6H, m),7.18-7.32 (4H, m), 7.51-7.66 (1H, m)

(21) MASS (m/z): 559 (M⁺ +1); NMR (CDCl₃, δ): 2.69 (3H×2/3, s), 2.95(3H×1/3, s), 3.00 (2H, m), 3.21 (2H, t, J=7 Hz), 4.22 (2H×1/3, s), 4.32(1H×2/3, d, J=15 Hz), 4.91 (1H×2/3, d, J=15 Hz), 5.31 (1H, m), 5.76 (1H,m), 6.92-7.15 (14H, m), 7.20-7.31 (5H, m), 7.48 (1H, d, J=8 Hz), 7.68(1H, d, J=8 Hz), 8.94 (1H, d, J=8 Hz)

(22) MASS (m/z): 660 (M⁺ +1); NMR (CDCl₃, δ): 1.60-1.70 (2H, m),1.80-1.98 (2H, m), 2.72 (3H×1/3, s), 2.78 (3H×2/3, s), 2.96-3.24 (4H,m), 4.23 (1H×1/3, d, J=15 Hz), 4.42 (1H×2/3, d, J=15 Hz), 4.63 (1H×1/3,d, J=15 Hz), 4.89 (1H×2/3, d, J=15 Hz), 5.02 (2H, s), 5.32-5.42 (2H, m),6.97-7.17 (10H, m), 7.21-7.31 (9H, m), 7.47 (1H, d, J=8 Hz), 7.68 (1H,dd, J=2, 8 Hz), 8.81 (1H, br s)

(23) MASS (m/z): 543 (M+H); NMR (CDCl₃, δ): 2.08 (3H, s), 2.10-2.32 (2H,m), 2.57-2.68 (2H, m), 2.72 (3×2/3H, s), 3.05 (3×1/3H, s), 3.00-3.07(2H, m), 4.16 (2×1/4H, d, J=17 Hz), 4.41 (2×1/4H, d, J=17 Hz), 4.50(2×1/4H, d, J=15 Hz), 4.89 (2×1/4H, d, J=15 Hz), 5.34-5.48 (1H, m),5.52-5.63 (1H, m), 6.98-7.18 (9H, m), 7.19-7.37 (5H, m), 7.49 (1H, d,J=8 Hz), 7.69 (1H, d, J=8 Hz), 9.08 (1H, , J=8 Hz)

(24) MASS (m/z): 560 (M+H); NMR (CDCl₃, δ): 2.02-2.26 (2H, m), 2.11 (3H,s), 2.57-2.63 (2H, m), 2.68 (3×2/3H, s), 2.89 (3×1/3H, s), 2.99-3.12(2H, m), 4.17 (2×1/4H, d, J=16 Hz), 4.41 (2×1/4H, d, J=16 Hz), 4.42(2×1/4H, d, J=15 Hz), 4.62 (2×1/4H, d, J=15 Hz), 4.90-5.01 (1H, m),5.17-5.27 (1H, m), 7.02-7.43 (13H, m), 7.59 (1H, t, J=8 Hz), 7.78-7.87(3H, m)

(25) MASS (m/z): 544 (M+H); NMR (CDCl₃, δ): 2.08 (3H, d, J=3 Hz),2.10-2.28 (2H, m), 2.53-2.63 (2H, m), 2.68 (3×2/3H, s), 2.92 (3×1/3H,s), 2.98-3.12 (2H, m), 4.19 (2×1/4H, d, J=16 Hz), 4.40 (2×1/4H, d, J=16Hz), 4.46 (2×1/4H, d, J=15 Hz), 4.63 (2×1/4H, d, J=15 Hz), 4.89-5.00(1H, m), 5.18-5.23 (1H, m), 7.02-7.18 (7H, m), 7.24-7.31 (4H, m),7.39-7.54 (5H, m), 7.69 (1H, d, J=8 Hz)

(26) MASS (m/z): 500 (M+1); NMR (CDCl₃, δ): 2.78 (3×2/3H, s), 2.91(3×1/3H, s), 2.95-3.13 (2H, m), 3.62-3.80 (2H, m), 3.88 (1H, t, J=8 Hz),4.03-4.17 (1H, m), 4.27-4.56 (2×2/3H, m), 4.69 (2×1/3H, d, J=15 Hz),4.72-4.79 (1H, m), 5.12-5.22 (1H, m), 7.04-7.18 (6H, m), 7.26-7.37 (3H,m), 7.40 (2H, t, J=8 Hz), 7.50 (1H, s), 7.52 (2H, t, J=8 Hz), 7.62 (1H,d, J=8 Hz)

(27) MASS (m/z): 515 (M⁺ +1); NMR (CDCl₃, δ): 2.50 (3H×3/4, s), 2.53(3H×1/4, s), 2.75 (3H×3/4, s), 2.83 (3H×1/4, s), 3.00-3.15 (2H, m), 3.81(1H, m), 4.10 (1H, m), 4.05-4.14 (2H×1/4, m), 4.44 (1H×3/4, d, J=15 Hz),4.50 (1H×3/4, d, J=15 Hz), 4.79 (1H, br s), 4.94 (1H, m), 5.18 (1H, m),7.00-7.18 (6H, m), 7.25-7.66 (7H, m), 7.88 (1H×1/4, d, J=8 Hz), 7.96(1H×3/4, d, J=8 Hz), 8.28 (1H, d, J=2 Hz)

(28) MASS (m/z): 514 (M⁺ +1); NMR (CDCl₃, δ): 2.41 (3H×6/7, s), 2.53(3H×1/7, s), 2.93 (3H, s), 3.10 (1H, dd, J=5, 12 Hz), 3.26 (1H, dd, J=7,12 Hz), 3.97 (2H, m), 4.28 (1H×6/7, d, J=15 Hz), 4.28 (1H×1/7, d, J=16Hz), 4.37 (1H×1/7, d, J=16 Hz), 4.78 (1H×6/7, d, J=15 Hz), 5.32 (1H, m),5.64 (1H, m), 6.69 (1H, d, J=8 Hz), 6.88 (1H×1/7, s), 6.92 (1H×6/7, s),7.04-7.25 (9H, m), 7.48 (1H, d, J=8 Hz), 7.61 (1H×1/7, d, J=8 Hz), 7.65(1H×6/7, d, J=8 Hz), 8.22 (1H, s), 9.22 (1H×1/7, d, J=8 Hz), 9.28(1H×6/7, d, J=8 Hz)

(29) MASS (m/z): 513 (M⁺ +1); NMR (CDCl₃, δ): 1.21 (3H×1/3, d, J=7 Hz),1.24 (3H×2/3, d, J=7 Hz), 2.76 (3H×2/3, s), 2.97 (3H×1/3, s), 3.00-3.14(2H, m), 3.92-4.83 (4H, m), 5.26-5.41 (2H, m), 7.02-7.14 (8H, m),7.16-7.31 (5H, m), 7.38-7.49 (2H, m), 7.65 (1H, d, J=8 Hz), 8.85(1H×1/3, d, J=8 Hz), 8.93 (1H×2/3, d, J=8 Hz)

(30) MASS (m/z): 514 (M⁺ +1); NMR (CDCl₃, δ): 1.16 (3H×1/3, d, J=7 Hz),1.21 (3H×2/3, d, J=7 Hz), 2.76 (3H×2/3, s), 2.93 (3H×1/3, s), 2.95-3.13(2H, m), 3.87-3.97 (1H, m), 4.28-4.75 (4H, m), 5.18 (1H, m), 7.05-7.16(6H, m), 7.21-7.32 (5H, m), 7.41-7.69 (5H, m)

(31) MASS: 609 (M+1); NMR (CDCl₃, δ): 2.42 (3×2/3H, s), 2.50 (3×1/3H,s), 2.82-3.08 (2H, m), 3.23-3.42 (2H, m), 3.47 (2×1/3H, d, J=15 Hz),3.70 (2×1/6H, d, J=16 Hz), 4.09 (2×1/6H, d, J=16 Hz), 4.70 (2×1/3H, d,J=15 Hz), 5.10-5.30 (1H, m), 5.80-6.00 (1H, m), 6.71-6.80 (2×1/3H, m),6.83-6.92 (2×2/3H, m), 6.93-7.30 (14H, m), 7.31-7.73 (7H, m), 8.97 (1H,d, J=8 Hz)

(32) MASS: 610 (M+1); NMR (CDCl₃, δ): 2.49 (3×2/3H, s), 2.68 (3×1/3H,s), 2.85-3.05 (2H, m), 3.22-3.48 (2H, m), 3.98 (2×1/3H, d, J=15 Hz),4.07 (2×1/3H, s), 4.58 (2×1/3H, d, J=15 Hz), 5.01-5.22 (2H, m),6.82-7.55 (19H, m), 7.60-7.70 (5H, m)

(33) MASS: 564 (M+1); NMR (CDCl₃, δ): 2.51 (3×1/4H, s), 2.52 (3×3/4H,s), 2.72 (3×3/4H, s), 2.83 (3×1/4H, s), 2.91-3.08 (2H, m), 3.10-3.28(2H, m), 4.18 (2×1/8H, d, J=16 Hz), 4.29 (2×1/8H, d, J=16 Hz), 4.30(2×3/8H, d, J=15 Hz), 4.72 (2×3/8H, d, J=15 Hz), 5.20-5.35 (1H, m),5.42-5.60 (1H, m), 6.69 (1×3/4H, s), 6.72 (1×1/4H, s), 6.90-7.20 (8H,m), 7.20-7.30 (2H, m), 7.32-7.58 (3H, m), 7.62 (1H, d, J=8 Hz), 8.15(1×1/4H, s), 8.21 (1×3/4H, s), 8.92 (1×3/4H, d, J=8 Hz), 9.00 (1×1/4H,d, J=8 Hz)

(34) MASS: 565 (M+1); NMR (CDCl₃, δ): 2.53 (3H, s), 2.60 (3×3/4H, s),2.78 (3×1/4H, s), 2.90-3.07 (2H, m), 3.08-3.33 (2H, m), 3.99 (2×1/8H, d,J=16 Hz), 4.31 (2×1/8H, d, J=16 Hz), 4.39 (2×3/8H, d, J=15 Hz), 4.49(2×3/8H, d, J=15 Hz), 4.95-5.18 (2H, m), 6.82 (1H, s), 7.00-7.30 (8H,m), 7.39 (1H, t, J=8 Hz), 7.43-7.58 (3H, m), 7.62 (1H, d, J=8 Hz), 8.00(1H, br s), 8.20 (1×1/4H, s), 8.28 (1×3/4H, s), 8.36 (1H, br s)

(35) MASS: 574 (M+1); NMR (CDCl₃, δ): 2.60-3.40 (4H, m), 2.71 (3H, s),2.91 (3H, s), 4.32-4.60 (2×2/3H, m), 4.67 (2×1/3H, s), 4.90-5.48 (2H,m), 6.85-7.48 (19H, m), 7.49-7.75 (2H, m)

(36) MASS: 573 (M+1); NMR (CDCl₃, δ): 2.72 (3×2/3H, s), 2.91 (3×1/3H,s), 2.85-3.14 (3H, m), 3.15-3.50 (1H, m), 3.29 (3×1/3H, s), 3.40(3×2/3H, s), 4.29 (2×1/3H, d, J=15 Hz), 4.33 (2×1/6H, d, J=16 Hz), 4.61(2×1/6H, d, J=16 Hz), 4.79 (2×1/3H, d, J=15 Hz), 5.13-5.30 (1H, m),4.48-4.58 (1×1/2H, m), 4.60-4.72 (1×1/2H, m), 6.70-6.82 (1H, m),6.85-7.20 (12H, m), 7.21-7.40 (5H, m), 7.40-7.60 (1H, m), 7.60-7.72 (1H,m), 8.07-8.17 (1×1/2H, m), 8.30-8.42 (1×1/2H, m)

(37) MASS: 612 (M+1); NMR (CDCl₃, δ): 2.67 (3×4/5H, s), 2.83 (3×1/5H,s), 2.88-3.08 (2H, m), 3.22-3.50 (2H, m), 4.32 (2×1/6H, d, J=16 Hz),4.48 (2×1/3H, d, J=15 Hz), 4.51 (2×1/6H, d, J=16 Hz), 4.78 (2×1/3H, d,J=15 Hz), 5.00-5.23 (2H, m), 7.00-7.21 (6H, m), 7.22-7.32 (2H, m),7.40-7.80 (8H, m), 7.91 (1H, s), 8.10 (1H, d, J=8 Hz), 8.23 (1×1/4H, d,J=8 Hz), 8.30 (1×3/4H, d, J=8 Hz), 8.52-8.70 (2H, m), 8.72 (1H, d, J=2Hz)

(38) MASS: 610 (M+1); NMR (CDCl₃, δ): 2.63 (3×2/3H, s), 2.80-3.10 (2H,m), 2.89 (3×1/3H, s), 3.30-3.43 (2H, m), 4.38 (2×1/6H, d, J=16 Hz), 4.43(2×1/6H, d, J=16 Hz), 4.59 (2×1/3H, d, J=15 Hz), 4.70 (2×1/3H, d, J=15Hz), 5.14-5.22 (1H, m), 5.23-5.49 (1H, m), 6.92-7.30 (11H, m), 7.32-7.58(3H, m), 7.62-7.80 (3H, m), 7.90 (1H, s), 8.08-8.28 (1H, m), 8.38-8.52(2H, m), 8.60 (1×1/4H, s), 8.72 (1×3/4H, s)

(39) MASS: 552 (M+1); NMR (CDCl₃, δ): 2.99-3.26 (2H, m), 3.00 (3H, s),3.70-3.83 (1H, m), 4.01-4.18 (1H, m), 4.25 (1H, br s), 4.79 (2×1/2H, d,J=15 Hz), 4.87-4.93 (1H, m), 4.97 (2×1/2H, d, J=15 Hz), 5.20-5.38 (1H,m), 7.03-7.20 (5H, m), 7.23-7.30 (1H, m), 7.40 (1H, t, J=8 Hz), 7.48(1H, d, J=8 Hz), 7.50 (1H, s), 7.58 (1H, d, J=8 Hz), 7.63 (1H, d, J=8Hz), 7.71-7.81 (3H, m), 7.97-8.05 (1H, m), 8.06-8.17 (1H, m), 8.80 (1H,s)

(40) MASS: 551 (M+1); NMR (CDCl₃, δ): 3.04-3.30 (2H, m), 3.08 (3H, s),3.90-4.08 (2H, m), 4.49 (2×1/6H, d, J=16 Hz), 4.62 (2×1/6H, d, J=16 Hz),4.79 (2×1/3H, d, J=15 Hz), 4.99 (2×1/3H, d, J=15 Hz), 5.20 (1H, br s),5.37-5.50 (1H, m), 5.60-5.73 (1H, m), 6.75 (1×1/4H, s), 6.81 (1×3/4H,s), 6.94-7.10 (4H, m), 7.12-7.22 (4H, m), 7.31 (1H, d, J=8 Hz),7.42-7.78 (4H, m), 7.98 (1H, d, J=8 Hz), 8.61 (1×1/4H, s), 8.69 (1×3/4H,s), 9.18 (1H, d, J=8 Hz)

(41) MASS: 613 (M+1); NMR (CDCl₃, δ): 2.80 (3×3/4H, s), 2.89-3.00 (2H,m), 2.94 (3×1/4H, s), 3.22-3.50 (2H, m), 4.60 (2×1/3H, d, J=15 Hz), 4.59(2×1/6H, d, J=16 Hz), 4.69 (2×1/6H, d, J=16 Hz), 4.93 (2×1/3H, d, J=15Hz), 5.00-5.30 (2H, m), 6.99-7.20 (6H, m), 7.22-7.32 (2H, m), 7.42 (1H,t, J=8 Hz), 7.47 (1H, s), 7.52-7.70 (3H, m), 7.72-7.80 (2H, m),7.94-8.03 (1H, m), 8.07-8.13 (1H, m), 8.27-8.39 (1H, m), 8.49-8.63 (2H,m), 8.63 (1×1/4H, s), 8.73 (1×3/4H, s)

(42) MASS: 612 (M+1); NMR (CDCl₃, δ): 2.80-3.12 (2H, m), 2.85 (3×3/4,s), 2.98 (3×1/4H, s), 3.26-3.40 (2H, m), 4.57 (2×1/6H, d, J=16 Hz), 4.70(2×1/6H, d, J=16 Hz), 4.71 (2×1/3H, d, J=15 Hz), 4.89 (2×1/3H, d, J=15Hz), 5.19-5.41 (2H, m), 6.90-7.23 (10H, m), 7.33-7.50 (2H, m), 7.63-7.80(3H, m), 7.97-8.03 (1H, m), 8.07-8.15 (1H, m), 8.22 (1×1/4H, d, J=8 Hz),8.33 (1×3/4H, d, J=8 Hz), 8.41 (1×3/4H, d, J=8 Hz), 8.50 (1H, d, J=5Hz), 8.61 (1×1/4H, s), 8.68 (1×1/4H, d, J=8 Hz), 8.70 (1×3/4H, s)

(43) MASS: 602 (M+1); NMR (CDCl₃, δ): 2.87 (3×4/5H, s), 2.94 (3×1/4H,s), 2.92-3.33 (4H, m), 4.68 (2×1/5H, s), 4.77 (2×2/5H, d, J=15 Hz), 4.83(2×2/5H, d, J=15 Hz), 4.92-5.30 (2H, m), 6.82 (1H, s), 7.00-7.20 (5H,m), 7.20-7.31 (2H, t, J=8 Hz), 7.38 (1H, t, J=8 Hz), 7.44-7.59 (3H, m),7.62 (1H, d, J=8 Hz), 7.70-7.82 (2H, m), 7.84-8.18 (2H, m), 8.22-8.40(1H, m), 8.87 (1H, s)

(44) MASS: 601 (M+1); NMR (CDCl₃, δ): 2.78-3.30 (4H, m), 2.90 (3×4/5H,s), 3.01 (3×1/5H, s), 4.57 (2×1/6H, d, J=16 Hz), 4.78 (2×1/6H, d, J=16Hz), 4.80 (2×1/3H, d, J=15 Hz), 4.88 (2×1/3H, d, J=15 Hz), 5.22-5.60(2H, m), 6.69 (1×4/5H, s), 6.71 (1×1/5H, s), 6.85-7.20 (8H, m),7.30-7.49 (2H, m), 7.57 (1H, t, J=8 Hz), 7.62-7.82 (3H, m), 7.92-8.02(1H, m), 8.03-8.12 (1H, m), 8.59 (1×1/5H, s), 8.67 (1×4/5H, s),8.90-9.18 (1H, m)

(45) MASS: 577 (M+1); NMR (CDCl₃, δ): 1.82 (1H, br s), 2.97 (3×1/4H, s),2.99 (3×3/4H, s), 3.07-3.19 (1H, m), 3.20-3.30 (1H, m), 3.90-4.19 (2H,m), 4.42 (2×1/3H, d, J=15 Hz), 4.50 (2×1/6H, d, J=16 Hz), 4.60 (2×1/6H,d, J=16 Hz), 4.80 (2×1/3H, d, J=15 Hz), 5.30-5.40 (1H, m), 5.56-5.70(1H, m), 6.51 (1×1/4H, s), 6.71 (1×3/4H, s), 7.03-7.40 (9H, m), 7.50(1H, d, J=8 Hz), 7.59 (1H, d, J=8 Hz), 7.73 (1H, d, J=8 Hz), 7.80 (1H,t, J=8 Hz), 8.08 (1H, d, J=8 Hz), 8.25-8.49 (2H, m), 8.67 (1×1/4H, d,J=2 Hz), 8.72 (1×3/4H, d, J=2 Hz), 9.10 (1×1/4H, d, J=8 Hz), 9.17(1×3/4H, d, J=8 Hz)

(46) MASS: 578 (M+1); NMR (CDCl₃, δ): 1.92 (1H, br s), 2.75 (3×3/4H, s),2.88 (3×1/4H, s), 2.98-3.18 (2H, m), 3.70-3.82 (1H, m), 4.07-4.20 (1H,m), 4.23 (2×1/6H, d, J=16 Hz), 4.50 (2×1/3H, d, J=15 Hz), 4.55 (2×1/6H,d, J=16 Hz), 4.68 (2×1/3H, d, J=15 Hz), 4.73-4.90 (1H, m), 5.12-5.28(1H, m), 7.10-7.36 (7H, m), 7.42 (1H, t, J=8 Hz), 7.47-7.70 (6H, m),7.81 (1H, t, J=8 Hz), 8.27-8.40 (2H, m), 8.49 (1×1/4H, s), 8.51 (1×3/4,s), 8.62-8.68 (1H, m)

(47) MASS: 638 (M+1); NMR (CDCl₃, δ): 2.68 (3×4/5H, s), 2.79-3.10 (2H,m), 2.85 (3×1/5H, s), 3.30-3.47 (2H, m), 4.19 (2×1/6 Hz, d, J=16 Hz),4.30 (2×1/6H, d, J=16 Hz), 4.43 (2×1/3H, d, J=15 Hz), 4.57 (2×1/3H, d,J=15 Hz), 5.11-5.28 (1H, m), 5.29-5.48 (1H, m), 6.90-7.14 (8H, m),7.15-7.30 (2H, m), 7.31-7.52 (4H, m), 7.52-7.60 (1H, m), 7.67 (1H, d,J=8 Hz), 8.22-8.38 (2H, m), 8.40-8.53 (3H, m), 8.60-8.72 (1H, m),9.10-9.22 (1H, m)

(48) MASS: 639 (M+1); NMR (CDCl₃, δ): 2.61 (3×4/5H, s), 2.80 (3×1/5H,s), 2.83-3.09 (2H, m), 3.28-3.50 (2H, m), 4.19 (2×1/6H, d, J=16 Hz),4.36 (2×1/6H, d, J=16 Hz), 4.40 (2×1/3H, d, J=15 Hz), 4.58 (2×1/3H, d,J=15 Hz), 5.02-5.22 (2H, m), 7.05-7.33 (8H, m), 7.35-7.50 (4H, m),7.51-7.70 (5H, m), 8.22 (1H, d, J=8 Hz), 8.28 (1H, d, J=8 Hz), 8.38(1×1/5H, s), 8.45 (1×4/5H, s), 8.56 (1H, d, J=2 Hz), 8.61 (1H, d, J=4Hz), 9.18 (1H, s)

(49) MASS: 578 (M+1); NMR (CDCl₃, δ): 2.80 (3×3/4H, s), 2.89 (3×1/4H,s), 3.00-3.19 (2H, m), 3.72-3.82 (1H, m), 4.08-4.20 (1H, m), 4.21-4.33(1H, m), 4.13 (2×1/6H, d, J=16 Hz), 4.24 (2×1/6H, d, J=16 Hz), 4.53(2×1/3H, d, J=15 Hz), 4.59 (2×1/3H, d, J=15 Hz), 4.78-4.90 (1H, m),5.12-5.28 (1H, m), 7.11-7.22 (5H, m), 7.23-7.33 (1H, m), 7.35-7.47 (3H,m), 7.48-7.60 (3H, m), 7.62-7.73 (3H, m), 8.30 (1H, t, J=7 Hz), 8.49(1×1/4H, s), 8.51 (1×3/4H, s), 8.65 (1H, br s), 9.17 (1H, br s)

(50) MASS (m/z): 781 (M⁺ +1); NMR (CDCl₃, δ): 1.30-1.57 (2H, m), 1.98(2H, m), 2.18 (3H, s), 2.65 (3H, s), 2.78 (2H, m), 2.85 (6H, s),3.04-3.23 (2H, m), 3.72-3.90 (2H, m), 3.85 (3H, s), 4.88-4.93 (2H, m),5.36 (1H, m), 6.42 (1H, m), 6.57 (1H, s), 7.03 (2H, d, J=8 Hz),7.14-7.32 (9H, m), 7.41 (1H, t, J=8 Hz), 7.47 (1H, s), 7.52 (1H, d, J=8Hz), 7.67 (1H, d, J=8 Hz)

(51) MASS (m/z): 561 (M⁺ +1); NMR (CDCl₃, δ): 2.60 (3H×3/4, s), 2.82(3H×1/4, s), 2.99 (2H, d, J=7 Hz), 3.20 (2H, m), 4.12 (1H×1/4, d, J=16Hz), 4.23 (1H×1/4, d, J=16 Hz), 4.34 (1H×3/4, d, J=15 Hz), 4.62 (1H×3/4,d, J=15 Hz), 5.03 (1H, m), 5.11 (1H, m), 7.09-7.15 (5H, m), 7.19-7.32(9H, m), 7.36-7.46 (2H, m), 7.52 (1H, d, J=8 Hz), 7.53 (1H, s), 7.67(1H, d, J=8 Hz), 8.30 (1H×1/4, br s), 8.41 (1H×3/4, br s), 8.53 (1H, brs)

(52) MASS (m/z): 560 (M⁺ +1); NMR (CDCl₃, δ): 2.69 (3H×3/4, s), 2.88(3H×1/4, s), 3.00 (2H, m), 3.20 (2H, m), 4.14 (1H×1/4, d, J=16 Hz), 4.25(1H×1/4, d, J=16 Hz), 4.28 (1H×3/4, d, J=15 Hz), 4.85 (1H×3/4, d, J=15Hz), 5.30 (1H, m), 5.73 (1H, m), 7.02-7.17 (14H, m), 7.20-7.31 (3H, m),7.45 (1H, d, J=8 Hz), 7.67 (1H, d, J=8 Hz), 8.29 (1H×1/4, br s), 8.43(1H×3/4, br s), 8.55 (1H, m), 8.88 (1H×3/4, d, J=7 Hz), 9.03 (1H×1/4, d,J=7 Hz)

(53) MASS (m/z): 562 (M⁺ +1); NMR (CDCl₃, δ): 2.62 (3H×3/4, s), 2.82(3H×1/4, s), 2.96 (2H, m), 3.17 (2H, m), 4.06 (1H×1/4, d, J=16 Hz), 4.27(1H×1/4, d, J=16 Hz), 4.35 (1H×3/4, d, J=15 Hz), 4.62 (1H×3/4, d, J=15Hz), 5.07 (2H, m), 7.04-7.17 (7H, m), 7.20-7.51 (6H, m), 7.65 (1H, d,J=8 Hz), 8.30-8.53 (4H, m)

(54) MASS (m/z): 561 (M⁺ +1); NMR (CDCl₃, δ): 2.68 (3H×3/4, s), 2.94(3H×1/4, s), 2.98 (2H, m), 3.20 (2H, m), 4.07 (1H×1/4, d, J=16 Hz), 4.22(1H×1/4, d, J=16 Hz), 4.30 (1H×3/4, d, J=15 Hz), 4.89 (1H×3/4, d, J=15Hz), 5.29 (1H, q, J=7 Hz), 5.83 (1H, q, J=7 Hz), 7.07-7.15 (10H, m),7.21-7.44 (4H, m), 7.67 (1H, d, J=8 Hz), 8.32-8.57 (4H, m), 8.91(1H×3/4, d, J=8 Hz), 9.03 (1H×1/4, d, J=8 Hz)

(55) MASS (m/z): 567 (M⁺ +1); NMR (CDCl₃, δ): 2.80 (3H×3/4, s), 2.88(3H×1/4, s), 3.08 (2H, m), 3.76 (1H, m), 4.07-4.18 (2H, m), 4.24 (1×1/4,d, J=16 Hz), 4.53 (1H×3/4, d, J=15 Hz), 4.53 (1H×1/4, d, J=16 Hz), 4.62(1H×3/4, d, J=15 Hz), 4.82 (1H, m), 5.21 (1H, q, J=7 Hz), 7.15-7.32 (7H,m), 7.42 (1H, t, J=8 Hz), 7.49-7.71 (7H, m), 8.10 (1H, s), 8.55 (1H×3/4,s), 8.58 (1H×1/4, s)

(56) MASS (m/z): 566 (M⁺ +1); NMR (CDCl₃, δ): 2.70 (3H×3/4, s), 2.83(3H×1/4, s), 3.09 (2H, m), 3.97 (2H, m), 4.01 (1H×1/4, d, J=16 Hz), 4.27(1H×1/4, d, J=16 Hz), 4.45 (1H×3/4, d, J=15 Hz), 4.60 (1H×3/4, d, J=15Hz), 5.36 (1H, m), 5.61 (1H, m), 6.90-7.22 (11H, m), 7.37-7.46 (3H, m),7.55 (1H×3/4, d, J=8 Hz), 7.62 (1H, d, J=8 Hz), 7.75 (1H×1/4, d, J=8Hz), 8.02 (1H×1/4, s), 8.06 (1H×3/4s), 8.46 (1H×3/4,s), 8.61 (1H×1/4,s), 9.00 (1H×3/4, d, J=8 Hz), 9.11 (1H×1/4, d, J=8 Hz)

(57) MASS (m/z): 559 (M+1)⁺ ; NMR (CDCl₃, δ): 2.04-2.21 (2H, m), 2.12(3H, s), 2.52 (3H, s), 2.61 (2H, m), 2.67 (3H×4/5, s), 2.81 (3H×1/5, s),3.02 (2H, d, J=7.0 Hz), 4.40 (1H, d, J=14.5 Hz), 4.54 (1H, d, J=14.5Hz), 4.84 (1H, m), 5.09-5.26 (1H, m), 6.98-7.08 (1H, m), 7.09-7.56 (12H,m), 7.69 (1H, d, J=7.5 Hz), 8.24 (1H×1/5, d, J=1.5 Hz), 8.33 (1H×4/5, d,J=1.5 Hz)

(58) MASS (m/z): 558 (M+1)⁺ ; NMR (CDCl₃, δ): 2.10 (3H, s), 2.19 (2H,m), 2.51-2.68 (2H, m), 2.56 (3H×1/4, s), 2.58 (3H×3/4, s), 2.76 (3H×3/4,s), 2.98 (3H×1/4, s), 3.03 (2H, d, J=7.5 Hz), 4.53 (1H, d, J=14.5 Hz),4.68 (1H, d, J=14.5 Hz), 5.29-5.49 (2H, m), 6.98-7.03 (1H, m), 7.04-7.19(9H, m), 7.22-7.37 (2H, m), 7.49 (1H, d, J=7.5 Hz), 7.70 (1H, d, J=7.5Hz), 8.26 (1H×1/4, d, J=1.5 Hz), 8.37 (1H×3/4, d, J=1.5 Hz), 8.64 (1H,br d, J=7.5 Hz)

(59) MASS (m/z): 545 (M+1)⁺ ; NMR (CDCl₃, δ): 2.06-2.21 (2H, m), 2.13(3H, s), 2.63 (2H, m), 2.70 (3H×3/4, s), 3.86 (3H×1/4, s), 3.03 (2H, d,J=7.5 Hz), 4.11 (1H×1/4, d, J=14.5 Hz), 4.39 (1H×1/4, d, J=14.5 Hz),4.42 (1H×3/4, d, J=14.5 Hz), 4.61 (1H×3/4, d, J=14.5 Hz), 4.87 (1H, m),5.13 (1H, m), 7.03-7.35 (9H, m), 7.40-7.58 (4H, m), 7.70 (1H, d, J=7.5Hz), 8.36 (1H×1/4, d, J=1.5 Hz), 8.44 (1H×3/4, d, J=1.5 Hz), 8.55 (1H,m)

(60) MASS (m/z): 544 (M+1)⁺ ; NMR (CDCl₃, δ): 2.10 (3H, s), 2.20 (2H,m), 2.63 (2H, m), 2.77 (3H×3/4, s), 2.99 (3H×1/4, s), 3.03 (2H, d, J=7.5Hz), 4.18 (1H×1/4, d, J=14.5 Hz), 4.52 (1H×1/4, d, J=14.5 Hz), 4.53(1H×3/4, d, J=14.5 Hz), 4.77 (1H×3/4, d, J=14.5 Hz), 5.39 (2H, m), 7.01(1H, m), 7.06-7.19 (7H, m), 7.20-7.34 (4H, m), 7.40-7.51 (2H, m), 7.70(1H, d, J=7.5 Hz), 8.35 (1H×1/4, s), 8.48 (1H×3/4, s), 8.53-8.68 (1H, m)

(61) MASS (m/z): 594 (M+1)⁺ ; NMR (CDCl₃, δ): 2.08 (3H×1/4, s), 2.10(3H×3/4, s), 2.11-2.29 (2H, m), 2.54-2.69 (2H, m), 2.83 (3H×3/4, s),3.02 (3H×1/4, s), 3.07 (2H, s), 4.37 (1H×1/4, d, J=14.5 Hz), 4.60(1H×1/4, d, J=14.5 Hz), 4.72 (1H×3/4, d, J=14.5 Hz), 4.91 (1H×3/4, d,J=14.5 Hz), 5.30-5.43 (2H, m), 6.97-7.20 (8H, m), 7.20-7.30 (1H, m),7.43-7.62 (3H, m), 7.65-7.83 (13/4H, m), 7.98 (1H×3/4, s), 8.09-8.19(1H, m), 8.52 (1H, d, J=7.5 Hz), 8.68 (1H×1/4, d, J=1.5 Hz), 8.82(1H×3/4, d, J=1.5 Hz)

(62) MASS (m/z): 595 (M+1)⁺ ; NMR (CDCl₃, δ): 2.07-2.26 (2H, m), 2.11(3H, s), 2.53-2.69 (2H, m), 2.73 (3H×4/5, s), 2.91 (3H×1/5, s),3.02-3.10 (2H, m), 4.30 (1H×1/5, d, J=14.5 Hz), 4.60 (1H×1/5, d, J=14.5Hz), 4.62 (1H×4/5, d, J=14.5 Hz), 4.78 (1H×4/5, d, J=14.5 Hz), 4.88 (1H,m), 5.18 (1H, m), 7.04-7.20 (6H, m), 7.23-7.37 (2H, m), 7.45 (1H, t,J=7.5 Hz), 7.49-7.62 (3H, m), 7.66-7.86 (16/5H, m), 7.99 (1H×4/5, s),8.13 (1H, d, J=7.5 Hz), 8.70 (1H×1/5, d, J=1.5 Hz), 8.80 (1H×4/5, d,J=1.5 Hz)

(63) MASS (m/z): 596 (M+1)⁺ ; NMR (CDCl₃, δ): 2.03-2.22 (2H, m), 2.11(3H, s), 2.52-2.67 (2H, m), 2.92 (3H×4/5, s), 3.00 (3H×1/5, s), 3.08(2H, t, J=7.5 Hz), 4.73 (1H, d, J=14.5 Hz), 4.79-4.90 (1H, m), 4.96 (1H,d, J=14.5 Hz), 5.16-5.28 (1H, m), 7.02-7.17 (6H, m), 7.21-7.36 (2H, m),7.43 (1H, t, J=7.5 Hz), 7.48-7.57 (2H, m), 7.69 (1H, d, J=7.5 Hz),7.73-7.81 (2H, m), 7.99-8.06 (1H, m), 8.10-8.15 (1H, m), 8.73 (1H×1/5,s), 8.82 (1H×4/5, s)

(64) MASS (m/z): 595 (M+1)⁺ ; NMR (CDCl₃, δ): 2.08 (3H, s), 2.10-2.27(2H, m), 2.57-2.69 (2H, m), 3.01 (3H×4/5, s), 3.03-3.10 (2H, m), 3.15(3H×1/5, s), 4.83 (1H, d, J=14.5 Hz), 5.09 (1H, d, J=14.5 Hz), 5.25-5.48(2H, m), 6.89-7.24 (10H, m), 7.33-7.40 (1H, m), 7.62-7.70 (1H, m),7.74-7.83 (2H, m), 8.01-8.08 (1H, m), 8.11-8.19 (1H, m), 8.39-8.47 (1H,m), 8.69 (1H×1/5, s), 8.83 (1H×4/5, s)

(65) MASS (m/z): 621 (M+1)⁺ ; NMR (CDCl₃, δ): 2.07 (3H, s), 2.10-2.33(2H, m), 2.59-2.68 (2H, m), 2.83 (3H×3/4, s), 3.02 (3H×1/4, s), 3.04(2H, d, J=7.5 Hz), 4.22 (1H×1/4, d, J=14.5 Hz), 4.46 (1H×1/4, d, J=14.5Hz), 4.63 (1H×3/4, d, J=14.5 Hz), 4.75 (1H×3/4, d, J=14.5 Hz), 5.33-5.49(2H, m), 6.99 (1H×1/4, d, J=1.5 Hz), 7.01 (1H×3/4, d, J=1.5 Hz),7.04-7.19 (7H, m), 7.23-7.32 (1H, m), 7.39-7.54 (3H, m), 7.67-7.73 (2H,m), 8.33 (1H, d, J=7.5 Hz), 8.45 (1H×1/4, d, J=1.5 Hz), 8.57 (1H×3/4, d,J=1.5 Hz), 8.63-8.88 (2H, m), 9.21 (1H, s), 10.32 (1H, br s)

(66) MASS (m/z): 622 (M+1)⁺ ; NMR (CDCl₃, δ): 2.04-2.26 (2H, m), 2.13(3H, s), 2.53-2.69 (2H, m), 2.74 (3H×4/5, s), 2.87 (3H×1/5, s),2.99-3.14 (2H, m), 4.16 (1H×1/5, d, J=14.5 Hz), 4.44 (1H×1/5, d, J=14.5Hz), 4.53 (1H×4/5, d, J=14.5 Hz), 4.61 (1H×4/5, d, J=14.5 Hz), 4.88 (1H,quint, J=7.5 Hz), 5.17 (1H, quint, J=7.5 Hz), 7.10-7.25 (6H, m),7.27-7.60 (7H, m), 7.66-7.74 (2H, m), 8.28-8.34 (1H, m), 8.44 (1H×1/5,d, J=1.5 Hz), 8.54 (1H×4/5, d, J=1.5 Hz), 8.68 (1H, d, J=5.5 Hz), 9.20(1H, m)

(67) MASS (m/z): 566 (M+1)⁺ ; NMR (CDCl₃, δ): 2.60 (3H×2/3, s), 2.87(3H×1/3, s), 3.00 (2H, t, J=7.5 Hz), 3.37-3.46 (2H, m), 4.06 (1H×1/3, d,J=14.5 Hz), 4.31 (1H×1/3, d, J=14.5 Hz), 4.41 (1H×2/3, d, J=14.5 Hz),4.56 (1H×2/3, d, J=14.5 Hz), 4.85-4.99 (1H, m), 5.10-5.21 (1H, m),6.83-7.21 (11H, m), 7.22-7.33 (5H, m), 7.43 (1H, t, J=7.5 Hz), 7.49-7.57(2H, m), 7.70 (1H, d, J=7.5 Hz)

(68) MASS (m/z): 565 (M+1)⁺ ; NMR (CDCl₃, δ): 2.69 (3H×2/3, s), 2.99(3H×1/3, s), 3.03 (2H, d, J=7.5 Hz), 3.49 (2H, t, J=7.5 Hz), 4.10(1H×1/3, d, J=14.5 Hz), 4.31 (1H×1/3, d, J=14.5 Hz), 4.43 (1H×2/3, d,J=14.5 Hz), 4.86 (1H×2/3, d, J=14.5 Hz), 5.22-5.37 (1H, m), 5.58-5.70(1H, m), 6.78-6.88 (2H, m), 6.93-7.20 (11H, m), 7.23-7.39 (5H, m), 7.51(1H, d, J=7.5 Hz), 7.70 (1H, m), 8.71 (1H, br d, J=7.5 Hz)

(69) MASS (m/z): 543 (M+H)⁺ ; NMR (CDCl₃, δ): 2.83 (3/4×3H, s), 2.91(1/4×3H, s), 2.95-3.30 (2H, m), 3.02 (3/4×6H, s), 3.06 (1/4×6H, s), 3.81(1/4×1H, d, J=17 Hz), 3.88-4.04 (2H, m), 4.24 (3/4×1H, d, J=15 Hz), 4.36(1/4×1H, d, J=17 Hz), 4.65 (3/4×1H, d, J=15 Hz), 5.18-5.64 (2H, m), 6.16(3/4×1H, d, J=9 Hz), 6.43 (1/4×1H, d, J=9 Hz), 6.88-7.92 (13H, m),8.88-9.12 (1H, m), 10.00 (1H, br s)

(70) MASS (m/z): 544 (M+H)⁺ ; NMR (CDCl₃, δ): 2.72 (2/3×3H, s), 2.82(1/3×3H, s), 2.91-3.12 (2H, m), 3.08 (6H, s), 3.63-3.80 (1H, m), 3.92(1/3×1H, d, J=17 Hz), 4.05-4.20 (1H, m), 4.39 (2/3×2H, ABq, Δ=0.13, J=15Hz), 4.42 (1/3×1H, d, J=17 Hz), 4.68-4.82 (1H, m), 5.04-5.32 (1H, m),6.48 (2/3×1H, d, J=9 Hz), 6.50 (1/3×1H, d, J=9 Hz), 7.06-7.73 (13H, m),7.94 (1/3×1H, d, J=2 Hz), 7.98 (2/3×1H, d, J=2 Hz)

(71) MASS (m/z): 567 (M+H)⁺ ; NMR (CDCl₃, δ): 2.80 (3/4×3H, s), 2.90(1/4×3H, s), 2.96-3.20 (2H, m), 3.50-3.85 (1H, m), 3.96-4.22 (1H, m),4.26 (1/4×1H, d, J=17 Hz), 4.55-4.88 (1H+1/4×1H, m), 4.70 (3/4×2H, s),5.05-5.35 (1H, m), 7.00-8.18 (17H, m), 8.75 (1H, s)

(72) MASS (m/z): 641 (M+H)⁺ ; NMR (CDCl₃, δ): 2.71 (3/4×3H, s), 2.88(1/4×3H, s), 2.92-3.15 (2H, m), 3.56-3.73 (1H, m), 3.95-4.08 (1H, m),4.44 (1/4×2H, ABq, Δ=0.20, J=17 Hz), 4.51 (3/4×1H, d, J=15 Hz), 4.62(2H, s), 4.72-4.90 (1H, m), 4.82 (3/4×1H, d, J=15 Hz), 5.10-5.32 (1H,m), 7.00-8.15 (22H, m), 8.64 (1/4×1H, d, J=2 Hz), 8.77 (3/4×1H, d, J=2Hz)

(73) MASS (m/z): 549 (M+H)⁺ ; NMR (CDCl₃, δ): 2.70 (2/3×3H, s),2.90-3.13 (4H, m), 2.99 (1/3×3H, s), 4.21 (1/3×2H, ABq, Δ=0.09, J=17Hz), 4.40 (2/3×1H, d, J=15 Hz), 4.89 (2/3×1H, d, J=15 Hz), 5.22-5.41(1H, m), 5.56-5.72 (1H, m), 6.24 (1/3×1H, s), 6.28 (2/3×1H, s),6.87-7.75 (18H, m), 8.84 (1H, d, J=9 Hz), 11.48 (1H, br s)

(74) MASS (m/z): 550 (M+H)⁺ ; NMR (CDCl₃, δ): 2.63 (2/3×3H, s), 2.88(1/3×3H, s), 2.92-3.10 (4H, m), 4.23 (1/3×2H, ABq, Δ=0.18, J=17 Hz),4.52 (2/3×2H, ABq, Δ=0.14, J=15 Hz), 4.83-4.98 (1H, m), 5.09-5.22 (1H,m), 6.27 (1/3×1H, s), 6.31 (2/3×1H, s), 6.92-7.73 (19H, m)

(75) MASS (m/z): 549 (M+H)⁺ ; NMR (CDCl₃, δ): 2.72 (2/3×3H, s),2.95-3.13 (2H, m), 2.97 (1/3×3H, s), 3.22-3.34 (2H, m), 4.23 (1/3×2H,ABq, Δ=0.16, J=17 Hz), 4.42 (2/3×1H, d, J=15 Hz), 4.83 (2/3×1H, d, J=15Hz), 5.23-5.40 (1H, m), 5.61-5.77 (1H, m), 6.04-6.22 (2H, m), 6.90-7.74(17H, m), 8.88 (1H, d, J=8 Hz), 11.38 (2/3×1H, br s), 11.40 (1/3×1H, brs)

(76) MASS (m/z): 550 (M+H)⁺ ; NMR (CDCl₃, δ): 2.59 (2/3×3H, s), 2.85(1/3×3H, s), 2.88-3.33 (4H, m), 4.20 (1/3×2H, ABq, Δ=0.23, J=17 Hz),4.48 (2/3×2H, ABq, Δ=0.16, J=15 Hz), 4.90-5.07 (1H, m), 5.07-5.25 (1H,m), 6.06-6.32 (2H, m), 6.88-7.72 (18H, m)

(77) MASS: 547 (M+1); NMR (CDCl₃, δ): 2.70 (3×3/4H, s), 2.80 (3×1/4H,s), 2.95-3.17 (2H, m), 3.71-3.85 (1H, m), 3.90 (3H, s), 3.98 (2×1/8H, d,J=16 Hz), 4.05-4.19 (1H, m), 4.28 (2×3/8H, d, J=15 Hz), 4.41 (2×1/8H, d,J=16 Hz), 4.57 (2×3/8H, d, J=15 Hz), 4.78-4.88 (1H, m), 5.08-5.18(1×3/4H, m), 5.20-5.28 (1×1/4H, m), 6.69 (1×3/4H, d, J=8 Hz), 6.70(1×1/4H, d, J=8 Hz), 7.05-7.21 (5H, m), 7.29-7.48 (4H, m), 7.69 (1H, d,J=7 Hz), 7.76-7.89 (3H, m), 7.90-8.00 (1H, m)

(78) MASS: 601 (M+1); NMR (CDCl₃, δ): 2.79 (3×3/4H, s), 2.88 (3×1/4H,s), 2.92-3.08 (2H, m), 3.10-3.33 (2H, m), 4.29 (2×1/8H, d, J=16 Hz),4.53 (2×1/8H, d, J=16 Hz), 4.60 (2×3/8H, d, J=15 Hz), 4.71 (2×3/8H, d,J=15 Hz), 4.98-5.22 (2H, m), 6.82 (1H, s), 7.00-7.20 (5H, m), 7.27 (1H,t, J=8 Hz), 7.39 (1H, t, J=8 Hz), 7.45-7.60 (4H, m), 7.61-7.80 (3H, m),7.91 (1H, s), 7.92-8.18 (1H, m), 8.09 (1H, d, J=8 Hz), 8.30-8.50 (1H,m), 8.67 (1×1/4H, s), 8.71 (1×3/4H, s)

(79) MASS: 600 (M+1); NMR (CDCl₃, δ): 2.78 (3×4/5H, s), 2.92 (3×1/5H,s), 2.97-3.10 (2H, m), 3.11-3.30 (2H, m), 4.47 (2×2/5H, d, J=15 Hz),4.50 (2×1/5H, s), 5.00 (2×2/5H, d, J=15 Hz), 5.33 (1H, q, J=8 Hz),5.43-5.60 (1H, m), 6.69 (1×4/5H, s), 6.79 (1×1/5H, s), 6.99 (1H, s),7.02-7.19 (6H, m), 7.22 (1H, d, J=8 Hz), 7.32-7.60 (4H, m), 7.61-7.80(3H, m), 7.89 (1H, s), 8.10 (1H, d, J=8 Hz), 8.61 (1×1/5H, s), 8.70(1×4/5H, s), 8.97 (1×4/5H, d, J=8 Hz), 9.11 (1×1/5H, d, J=8 Hz)

(80) MASS: 628 (M+1); NMR (CDCl₃, δ): 2.70 (3×4/5H, s), 2.82 (3×1/5H,s), 2.90-3.10 (2H, m), 3.11-3.36 (2H, m), 4.12 (2×1/8H, d, J=16 Hz),4.41 (2×1/8H, d, J=16 Hz), 4.43 (2×3/8H, d, J=15 Hz), 4.60 (2×3/8H, d,J=15 Hz), 4.96-5.20 (2H, m), 6.88 (1H, s), 7.05-7.31 (6H, m), 7.32-7.43(2H, m), 7.44-7.70 (6H, m), 7.90-8.10 (1H, m), 8.20-8.33 (2H, m), 8.40(1×1/5H, s), 8.47 (1×4/5H, s), 8.61 (1H, d, J=2 Hz), 9.13 (1H, s)

(81) MASS: 627 (M+1); NMR (CDCl₃, δ): 2.77 (3×2/3H, s), 2.90 (3×1/3H,s), 2.92-3.10 (2H, m), 3.10-3.30 (2H, m), 4.40 (2×1/2H, d, J=15 Hz),4.79 (2×1/2H, d, J=15 Hz), 5.22-5.37 (1H, m), 5.38-5.50 (1H, m), 6.78(1H, s), 6.92-7.30 (8H, m), 7.32-7.80 (7H, m), 8.22 (1H, d, J=5 Hz),8.38 (1×1/3H, s), 8.46 (1×2/3H, s), 8.62 (1H, d, J=2 Hz), 8.70-8.90 (1H,m), 9.14 (1H,

(82) MASS: 589 (M+1); NMR (CDCl₃, δ): 2.69 (3×2/3H, s), 2.90 (3×1/3H,s), 2.95-3.05 (2H, m), 3.06-3.22 (2H, m), 3.39 (3×1/3H, s), 3.40(3×2/3H, s), 4.20 (2×1/6H, d, J=16 Hz), 4.21 (2×1/3H, d, J=15 Hz), 4.27(2×1/6H, d, J=16 Hz), 4.97 (2×1/3H, d, J=15 Hz), 5.20-5.40 (1H, m),5.61-5.80 (1H, m), 6.45-5.60 (2H, m), 6.88-7.15 (10H, m), 7.16-7.40 (6H,m), 7.49 (1H, d, J=8 Hz), 7.68 (1H, d, J=8 Hz), 8.95 (1H, d, J=8 Hz)

(83) MASS: 590 (M+1); NMR (CDCl₃, δ): 2.59 (3×2/3H, s), 2.85 (3×1/3H,s), 2.90-3.04 (2H, m), 3.05-3.19 (2H, m), 3.70 (3H, s), 4.12 (2×1/6H, d,J=16 Hz), 4.28 (2×1/6H, d, J=16 Hz), 4.35 (2×1/3H, d, J=15 Hz), 4.63(2×1/3H, d, J=15 Hz), 4.92-5.03 (1H, m), 5.07-5.20 (1H, m), 6.70-6.78(2H, m), 6.91-7.20 (10H, m), 7.21-7.33 (5H, m), 7.41 (1H, t, J=8 Hz),7.44-7.55 (2H, m), 7.68 (1H, d, J=8 Hz)

(84) MASS: 613 (M+1); NMR (CDCl₃, δ): 2.69 (3×3/4H, s), 2.85 (3×1/4H,s), 2.90-3.07 (2H, m), 3.35-3.50 (2H, m), 4.40 (2×1/8H, d, J=16 Hz),4.51 (2×1/8H, d, J=16 Hz), 4.58 (2×3/8H, d, J=15 Hz), 4.78 (2×3/8H, d,J=15 Hz), 5.01-5.22 (1H, m), 7.03-7.21 (5H, m), 7.22-7.35 (3H, m),7.37-7.50 (3H, m), 7.51-7.71 (4H, m), 7.72 (1×1/4H, s), 7.81 (1×3/4H,s), 7.99 (1H, t, J=8 Hz), 8.22-8.33 (1H, m), 8.49-8.69 (2H, m), 8.82(2H, s)

(85) MASS: 610 (M+1); NMR (CDCl₃, δ): 2.48 (3×2/3H, s), 2.78 (3×1/3H,s), 2.80-2.97 (2H, m), 3.42-3.60 (1H, m), 3.66-3.80 (1H, m), 4.07(2×1/6H, d, J=16 Hz), 4.11 (2×1/3H, d, J=15 Hz), 4.17 (2×1/6H, d, J=16Hz), 4.58 (2×1/3H, d, J=15 Hz), 4.90-5.10 (2H, m), 6.48-6.60 (1H, m),6.90-7.20 (7H, m), 7.21-7.60 (12H, m), 7.61-7.78 (2H, m), 7.79-7.85 (1H,m), 8.23-8.37 (1H, m)

(86) MASS: 609 (M+1); NMR (CDCl₃, δ): 2.52 (3×2/3H, s), 2.75-3.00 (2H,m), 2.83 (3×1/3H, s), 3.08-3.30 (1H, m), 3.52-3.68 (1H, m), 3.95(2×1/6H, d, J=16 Hz), 4.09 (2×1/3H, d, J=15 Hz), 4.17 (2×1/6H, d, J=16Hz), 4.90 (2×1/3H, d, J=15 Hz), 5.10-5.23 (1H, m), 5.59-5.80 (1H, m),6.83-7.35 (18H, m), 7.40-7.60 (3H, m), 7.71 (1H, d, J=8 Hz), 7.88(1×1/3H, d, J=8 Hz), 7.92 (1×2/3H, d, J=8 Hz), 8.91 (1H, d, J=7 Hz)

(87) MASS: 550 (M+1); NMR (CDCl₃, δ): 2.71 (3×4/5H, s), 2.82 (3×1/5H,s), 2.89-3.08 (2H, m), 3.09-3.30 (2H, m), 4.22 (2×1/10H, d, J=16 Hz),4.31 (2×1/10H, d, J=16 Hz), 4.38 (2×2/5H, d, J=15 Hz), 4.70 (2×2/5H, d,J=15 Hz), 5.19-5.39 (1H, m), 5.42-5.59 (1H, m), 6.69 (1×4/5H, s), 6.72(1×1/5H, s), 6.97-7.30 (9H, m), 7.31 (1H, d, J=8 Hz), 7.39-7.59 (3H, m),7.62 (1H, d, J=8 Hz), 8.22 (1×1/5H, s), 8.33 (1×4/5H, s), 8.44-8.55 (1H,m), 8.88-9.10 (1H, m)

(88) MASS: 551 (M+1); NMR (CDCl₃, δ): 2.61 (3×4/5H, s), 2.78 (3×1/5H,s), 2.90-3.07 (2H, m), 3.08-3.33 (2H, m), 4.09 (2×1/10H, d, J=16 Hz),4.34 (2×1/10H, d, J=16 Hz), 4.42 (2×2/5H, d, J=15 Hz), 4.51 (2×2/5H, d,J=15 Hz), 4.95-5.15 (2H, m), 6.81 (1H, s), 7.05-7.32 (7H, m), 7.39 (2H,t, J=8 Hz), 7.47-7.60 (3H, m), 7.62 (1H, d, J=8 Hz), 8.01 (1H, d, J=5Hz), 8.29 (2×1/5H, s), 8.37 (2×4/5H, s), 8.48 (1H, d, J=3 Hz)

(89) MASS: 575 (M+1); NMR (CDCl₃, δ): 2.51 (3H, s), 2.61 (3×3/4H, s),2.79 (3×1/4H, s), 2.81-3.07 (2H, m), 3.25-3.45 (2H, m), 4.08 (2×1/8H, d,J=16 Hz), 4.21 (2×1/8H, d, J=16 Hz), 4.36 (2×3/8H, d, J=15 Hz), 4.51(2×3/8H, d, J=15 Hz), 5.08-5.28 (1H, m), 5.30-5.50 (1H, m), 6.93-7.30(13H, m), 7.32-7.50 (2H, m), 7.69 (1H, d, J=8 Hz), 8.18 (1×1/4H, s),8.30 (1×3/4H, s), 8.22 (1×1/4H, d, J=8 Hz), 8.39 (1×3/4H, d, J=8 Hz),8.49 (1×3/4H, d, J=8 Hz), 8.67 (1×1/4H, d, J=8 Hz)

(90) MASS: 576 (M+1); NMR (CDCl₃, δ): 2.50 (3H, s), 2.55 (3×3/4H, s),2.72 (3×1/4H, s), 2.78-3.02 (2H, m), 3.22-3.38 (1H, m), 3.38-3.50 (1H,m), 4.01 (2×1/8H, d, J=16 Hz), 4.22 (2×3/8H, d, J=15 Hz), 4.23 (2×1/8H,d, J=16 Hz), 4.51 (2×3/8H, d, J=15 Hz), 5.00-5.20 (2H, m), 6.98-7.37(10H, m), 7.38-7.50 (2H, m), 7.50-7.70 (3H, m), 8.12-8.20 (1H, m), 8.18(1×1/4H, s), 8.22 (1×3/4H, s), 8.50-8.68 (2H, m)

(91) MASS: 560 (M+1); NMR (CDCl₃, δ): 2.78 (3×2/3H, s), 2.94 (3×1/3H,s), 2.88-3.10 (2H, m), 3.10-3.30 (2H, m), 4.29 (2×1/3H, d, J=15 Hz),4.31 (2×1/3H, s), 4.99 (2×1/3H, d, J=15 Hz), 5.17-5.40 (1H, m),5.70-5.90 (1H, m), 6.84-6.94 (2H, m), 6.95-7.15 (8H, m), 7.16-7.33 (5H,m), 7.34-7.60 (2H, m), 7.60-7.70 (1H, m), 8.23 (1H, s), 8.43 (1H, s),8.97 (1H, d, J=8 Hz)

(92) MASS: 561 (M+1); NMR (CDCl₃, δ): 2.62 (3×2/3H, s), 2.91 (3×1/3H,s), 2.88-3.30 (4H, m), 4.26 (2×1/6H, d, J=16 Hz), 4.33 (2×1/6H, d, J=16Hz), 4.37 (2×1/3H, d, J=15 Hz), 4.70 (2×1/3H, d, J=15 Hz), 4.62-4.75(2H, m), 6.92-7.20 (8H, m), 7.20-7.35 (4H, m), 7.35-7.73 (7H, m),8.35-8.50 (2H, m)

(93) MASS: 594 (M+1); NMR (CDCl₃, δ): 2.61 (3×2/3H, s), 2.89 (3×1/3H,s), 2.92-3.05 (2H, m), 3.09-3.23 (2H, m), 4.09 (2×1/6H, d, J=16 Hz),4.30 (2×1/6H, d, J=16 Hz), 4.39 (2×1/3H, d, J=15 Hz), 4.67 (2×1/3H, d,J=15 Hz), 4.98-5.21 (2H, m), 6.93-7.20 (11H, m), 7.21-7.38 (6H, m), 7.42(1H, t, J=8 Hz), 7.48-7.60 (2H, m), 7.68 (1H, d, J=8 Hz)

(94) MASS: 593 (M+1); NMR (CDCl₃, δ): 2.68 (3×2/3H, s), 2.88-3.04 (2H,m), 2.99 (3×1/3H, s), 3.07-3.23 (2H, m), 4.09 (2×1/6H, d, J=16 Hz), 4.22(2×1/6H, d, J=16 Hz), 4.25 (2×1/3H, d, J=15 Hz), 5.00 (2×1/3H, d, J=15Hz), 5.22-5.38 (1H, m), 5.68-5.83 (1H, m), 6.90-7.16 (13H, m), 7.17-7.40(5H, m), 7.49 (1H, d, J=8 Hz), 7.68 (1H, d, J=8 Hz), 8.91 (1H, d, J=8Hz)

(95) MASS: 572 (M+1); NMR (CDCl₃, δ): 2.40-3.00 (2H, m), 2.57 (3H, s),3.01-3.22 (1H, m), 3.30-3.47 (1H, m), 4.20-4.62 (1H, m), 4.30 (2×1/2H,d, J=15 Hz), 4.68 (2×1/2H, d, J=15 Hz), 4.90-5.20 (2H, m), 5.21-5.36(1H, m), 6.80-7.37 (16H, m), 7.38-7.60 (2H, m), 7.62-7.78 (2H, m)

(96) MASS: 571 (M+1); NMR (CDCl₃, δ): 2.50-3.30 (2H, m), 2.89 (3H, s),2.35-2.60 (1H, m), 4.20-4.40 (1H, m), 4.48 (2×1/2H, d, J=16 Hz),4.60-4.80 (1H, m), 4.76 (2×1/2H, d, J=16 Hz), 4.85-5.30 (2H, m),5.45-5.60 (1H, m), 6.20-6.60 (1H, m), 6.61-7.60 (18H, m), 8.60-8.90 (1H,m)

(97) MASS: 575 (M+1); NMR (CDCl₃, δ): 2.07 (3H, s), 2.11-2.25 (2H, m),2.50 (3H, s), 2.56-2.73 (2H, m), 2.63 (3×2/3H, s), 2.80 (3×1/3H, s),2.91-3.12 (2H, m), 4.01 (2×1/6H, d, J=16 Hz), 4.37 (2×1/6H, d, J=16 Hz),4.38 (2×1/3H, d, J=15 Hz), 4.52 (2×1/3H, d, J=15 Hz), 4.87-5.00 (1H, m),5.07-5.30 (1H, m), 7.00-7.22 (6H, m), 7.23-7.50 (4H, m), 7.59 (1×2/3H,d, J=8 Hz), 7.67 (1×1/3H, d, J=8 Hz), 7.70-7.90 (3H, m), 8.22 (1×1/3H,s), 8.29 (1×2/3H, s)

EXAMPLE 27

The following object compound was obtained according to a similar mannerto that of Example 8.

MASS (m/z): 575 (M+H)⁺ ; NMR (CDCl₃, δ): 2.67 (2/3×3H, s), 2.90-3.15(4H, m), 2.92 (1/3×3H, s), 4.28 (2/3×1H, d, J=15 Hz), 4.38 (1/3×1H, d,J=17 Hz), 4.64 (1/3×1H, d, J=17 Hz), 4.91 (2/3×1H, d, J=15 Hz),5.20-5.70 (2H, m), 6.05-7.70 (22H, m), 8.70 (1H, s)

EXAMPLE 28

The following object compound was obtained according to a similar mannerto that of Preparation 10.

MASS (m/z): 499 (M⁺ +1); NMR (CDCl₃, δ): 2.62 (3H×2/3, s), 2.85(3H×1/3s), 2.94-3.14 (2H, m), 3.79-4.08 (2H, m), 4.04 (1H×2/3, d, J=15Hz), 4.28 (1H×1/3, d, J=15 Hz), 4.39 (1H×1/3, d, J=15 Hz), 4.92 (1H×2/3,d, J=15 Hz), 5.25-5.62 (2H, m), 6.92-7.13 (9H, m), 7.16-7.27 (3H, m),7.42 (1H, m), 7.49-7.67 (2H, m), 8.67 (1H, m)

EXAMPLE 29

The following object compounds were obtained according to a similarmanner to that of Preparation 10.

(1) MASS (m/z): 540 (M⁺ +1); NMR (CDCl₃, δ): 1.24-1.96 (6H, m), 2.68(3H×1/3, s), 2.70 (3H×2/3, s), 2.83-3.18 (4H, m), 4.22-4.83 (2H, m),5.03-5.32 (2H, m), 6.78-7.60 (15H, m), 8.15 (2H, m)

(2) MASS (m/z): 526 (M⁺ +1); NMR (CDCl₃, δ): 1.92 (4H, m), 2.72 (3H×2/3,s), 2.91 (3H×1/3, s), 2.83-3.09 (4H, m), 4.24 (1H×2/3, d, J=15 Hz), 4.47(1H×2/3, d, J=15 Hz), 4.65 (1H×1/3, d, J=15 Hz), 4.85 (1H×2/3, d, J=15Hz), 5.27-5.38 (2H, m), 6.85-7.26 (14H, m), 7.42 (1H, d, J=8 Hz), 7.55(1H, d, J=8 Hz), 9.12 (1H, br s)

EXAMPLE 30

The following compounds were obtained according to a similar manner tothat of Example 3.

(1) MASS: 626 (M+1); NMR (CDCl₃, δ): 0.89 (4H, t, J=8 Hz), 0.99 (2H, t,J=8 Hz), 2.29-2.56 (6H, m), 2.62-2.83 (2H, m), 2.75 (3×2/3H, s), 2.99(3×1/3H, s), 3.02-3.12 (2H, m), 3.88-4.45 (2H, m), 4.63-4.72 (1H, m),4.92 (1H, dd, J=15, 8 Hz), 5.32-5.70 (2H, m), 6.98-7.18 (9H, m),7.20-7.36 (5H, m), 7.46 (1H, d, J=8 Hz), 7.68-7.71 (1H, m), 8.89(1×1/3H, t, J=8 Hz), 9.17 (1×2/3H, d, J=8 Hz)

(2) MASS: 601 (M+1); NMR (CDCl₃, δ): 2.29 (6H, s), 2.67 (3×2/3H, s),2.90 (3×1/3H, s), 3.00-3.10 (2H, m), 3.22-3.23 (2H, m), 3.28-3.39 (2H,m), 4.21 (2×1/6H, d, J=16 Hz), 4.38 (2×1/3H, d, J=15 Hz), 4.41 (2×1/6H,d, J=16 Hz), 4.70 (2×1/3H, d, J=15 Hz), 4.83-4.96 (1H, m), 5.12-5.22(1H, m), 7.00-7.19 (7H, m), 7.23-7.32 (4H, m), 7.40-7.70 (6H, m)

(3) MASS: 617 (M+1); NMR (CDCl₃, δ): 2.31 (6H, s), 2.63 (3×2/3H, s),2.89 (3×1/3H, s), 2.99-3.09 (2H, m), 3.11-3.43 (4H, m), 4.20 (2×1/6H, d,J=16 Hz), 4.37 (2×1/3H, d, J=15 Hz), 4.42 (2×1/6H, d, J=16 Hz), 4.69(2×1/3H, d, J=15 Hz), 4.72-4.80 (1H, m), 5.10-5.22 (1H, m), 7.00-7.20(8H, m), 7.21-7.35 (4H, m), 7.38-7.46 (2H, m), 7.72 (1×1/3H, s), 7.77(1×2/3H, s), 7.83-7.88 (2H, m)

(4) MASS (m/z): 619 (M+1); NMR (CDCl₃, δ): 2.63 (3×2/3H, s), 2.87(3×1/3H, s), 2.97-3.12 (2H, m), 3.62 (2H, s), 4.08-4.43 (2×2/3H, m),4.32-4.41 (1H, m), 4.48-4.58 (1H, m), 4.65 (2×1/3H, d, J=15 Hz),5.10-5.28 (2H, m), 6.98-7.20 (8H, m), 7.22-7.32 (5H, m), 7.39-7.49 (2H,m), 7.5.7 (2H, t, J=8 Hz), 7.69 (1H, d, J=8 Hz), 7.71 (1×2/3H, d, J=8Hz), 7.79 (1×1/3H, d, J=8 Hz), 8.42 (1H, br s), 8.47 (1H, br s)

(5) MASS (m/z): 605 (M+1); NMR (CDCl₃, δ): 2.62 (3×2/3H, s), 2.80(3×1/3H, s), 3.00-3.13 (2H, m), 4.08-4.40 (2×2/3H, m), 4.62 (2×1/3H, d,J=15 Hz), 4.63-4.72 (1H, m), 4.81-4.92 (1H, m), 5.20-5.33 (2H, m),6.91-7.30 (11H, m), 7.42 (2H, t, J=7 Hz), 7.50 (2H, d, J=10 Hz), 7.66(1H, d, J=8 Hz), 7.72-7.91 (3H, m), 8.10 (1H, t, J=8 Hz), 8.71 (1H, d,J=2 Hz)

(6) MASS (m/z): 584 (M+H)⁺ ; NMR (CDCl₃, δ): 2.23 (6H, s), 2.73 (3×2/3H,s), 3.00 (3×1/3H, s), 2.98-3.10 (2H, m), 3.13-3.22 (2H, m), 4.20(2×1/4H, d, J=16 Hz), 4.42 (2×1/4H, d, J=16 Hz), 4.43 (2×1/4H, d, J=15Hz), 4.94 (2×1/4H, d, J=15 Hz), 4.32-4.45 (1H, m), 4.68-4.80 (1H, m),5.35-5.46 (1H, m), 5.75-5.88 (1H, m), 6.99-7.22 (10H, m), 7.23-7.38 (4H,m), 7.50 (1H, d, J=8 Hz), 7.70 (1H, d, J=8 Hz), 9.16 (1H, d, J=8 Hz)

(7) MASS (m/z): 619 (M+1); NMR (CDCl₃, δ): 2.65 (3×2/3H, s), 2.88(3×1/3H, s), 2.99-3.12 (2H, m), 3.61 (2H, s), 4.10-4.42 (2×2/3H, m),4.36-4.43 (1H, m), 4.49-4.58 (1H, m), 4.71 (2×1/3H, d, J=15 Hz),5.09-5.29 (2H, m), 6.99-7.20 (9H, m), 7.22-7.38 (4H, m), 7.42 (2H, t,J=8 Hz), 7.52 (1H, s), 7.57 (1H, d, J=5 Hz), 7.63-7.73 (2H, m), 8.45(2H, br s)

(8) MASS (m/z): 605 (M+1); NMR (CDCl₃, δ): 2.62 (3×2/3H, s), 2.82(3×1/3H, s), 3.07 (2H, t, J=8 Hz), 4.08-4.38 (2×2/3H, m), 4.61 (2×1/3H,d, J=15 Hz), 4.63-4.78 (2H, m), 5.22-5.31 (1H, m), 5.33-5.40 (1H, m),6.91-7.32 (11H, m), 7.42 (1H, t, J=8 Hz), 7.52-7.61 (3H, m), 7.68 (1H,d, J=8 Hz), 7.73-7.80 (2H, m), 7.92 (1×2/3H, d, J=8 Hz), 8.01 (1×1/3H,d, J=8 Hz), 8.70 (2H, br s)

(9) MASS (m/z): 619 (M+1); NMR (CDCl₃, δ): 2.59 (3×2/3H, s), 2.80(3×1/3H, s), 2.91 (2H, t, J=8 Hz), 3.89 (2H, s), 4.08-4.34 (2×2/3H, m),4.53-4.60 (2H, m), 4.62 (2×1/3H, d, J=15 Hz), 5.00-5.10 (1H, m),5.13-5.22 (1H, m), 6.93-7.20 (13H, m), 7.40-7.48 (2H, m), 7.52 (1H, s),7.58-7.62 (2H, m), 7.68 (1H, d, J=8 Hz), 7.83 (1H, t, J=8 Hz), 8.57 (1H,d, J=2 Hz)

(10) MASS (m/z): 639 (M+1); NMR (CDCl₃, δ): 1.31-1.62 (6H, m), 2.30-2.43(4H, m), 2.50-2.57 (2H, m), 2.60-2.71 (2H, m), 2.63 (3×2/3H, s), 2.88(3×1/3H, s), 2.97-3.13 (2H, m), 4.13-4.69 (4H, m), 5.01-5.11 (1H, m),5.16-5.25 (1H, m), 6.98-7.20 (8H, m), 7.23-7.32 (2H, m), 7.40-7.70 (7H,m)

(11) MASS (m/z): 627 (M+1); NMR (CDCl₃, δ): 1.00 (6H, t, J=8 Hz),2.48-2.57 (7H, m), 2.62 (3×2/3H, s), 2.82 (2H, t, J=8 Hz), 2.89 (3×1/3H,s), 3.04 (2H, t, J=8 Hz), 4.05-4.69 (3H, m), 4.89-5.00 (1H, m),5.14-5.22 (1H, m), 7.00-7.22 (8H, m), 7.25-7.36 (4H, m), 7.44 (2H, q,J=8 Hz), 7.53 (1H, s), 7.56 (1H, dd, J=8, 2 Hz), 7.70 (1H, d, J=8 Hz)

(12) MASS (m/z): 585 (M+1); NMR (CDCl₃, δ): 2.28 (6H, s), 2.68 (3×2/3H,s), 2.91 (3×1/3H, s), 2.97-3.12 (2H, m), 3.17 (2H, d, J=8 Hz), 4.14-4.70(4H, m), 5.09-5.27 (2H, m), 6.97-7.22 (7H, m), 7.24-7.32 (4H, m), 7.43(1H, t, J=8 Hz), 7.49-7.58 (3H, m), 7.67-7.78 (2H, m)

EXAMPLE 31

Starting Compound (620 mg) was dissolved in methylenechloride (10 ml),and the solution was ice-cooled. To this solution was addedtrifluoroacetic acid (5 ml) and triethylsilane (476 mg). The mixture wasstirred at this temperature for ten minutes and at ambient temperaturefor one hour and was concentrated under reduced pressure. The residuewas dissolved in ethyl acetate and the organic layer was washed withsodium hydrogencarbonate solution and brine. After evaporation, thecrude material obtained was purified on a column of silica gel elutingwith chloroform-methanol (60:1) to give Object Compound (380 mg) as anamorphous solid.

MASS: 516 (M+1); NMR (CDCl₃, δ): 2.72 (3×2/3H, s), 2.78-2.88 (1H, m),2.89 (3×1/3H, s), 2.99-3.18 (3H, m), 4.22 (2×1/6H, d, J=16 Hz), 4.41(2×1/6H, d, J=16 Hz), 4.45 (2×1/3H, d, J=15 Hz), 4.63 (2×1/3H, d, J=15Hz), 4.87-4.97 (1H, m), 5.21 (1H, q, J=8 Hz), 7.03-7.19 (7H, m),7.26-7.35 (5H, m), 7.42-7.57 (4H, m), 7.69 (1H, d, J=8 Hz)

EXAMPLE 32

The following object compounds were obtained according to a similarmanner to that of Example 31.

(1) MASS: 532 (M+1); NMR (CDCl₃, δ): 2.73 (3×2/3H, s), 2.78-2.90 (1H,m), 2.90 (3×1/3H, s), 2.99-3.18 (3H, m), 4.18 (2×1/6H, d, J=16 Hz), 4.43(2×1/6H, d, J=16 Hz), 4.45 (2×1/3H, d, J=15 Hz), 4.61 (2×1/3H, d, J=15Hz), 4.81-4.92 (1H, m), 5.17-5.27 (1H, m), 7.03-7.20 (7H, m), 7.22-7.47(7H, m), 7.81-7.89 (3H, m)

(2) MASS: 515 (M+1); NMR (CDCl₃, δ): 2.77 (3×2/3H, s), 2.91-3.18 (4H,m), 3.03 (3×1/3H, s), 4.13 (2×1/6H, d, J=16 Hz), 4.41 (2×1/6H, d, J=16Hz), 4.51 (2×1/3H, d, J=15 Hz), 4.86 (2×1/3H, d, J=15 Hz), 5.37-5.52(1H, m), 5.63-5.73 (1H, m), 7.00-7.20 (9H, m), 7.22-7.40 (5H, m), 7.49(1H, d, J=8 Hz), 7.70 (1H, d, J=8 Hz), 9.11 (1H, t, J=8 Hz)

EXAMPLE 33

To a stirred solution of Starting Compound (0.11 g) and triethylamine(0.05 ml) in methylene chloride (5 ml) was added dropwise acetylchloride (0.02 g) at 0° C. and the mixture was stirred at roomtemperature for 1 hour. The reaction mixture was washed with 1N aqueoushydrochloric acid and 5% aqueous sodium bicarbonate, and dried.Evaporation of solvent gave a residue which was purified by columnchromatography on silica gel. Elution with chloroform ˜3%methanol-chloroform afforded Object Compound (0.05 g) as powder.

MASS (m/z): 582 (M⁺ +1); NMR (CDCl₃, δ): 1.41-1.94 (6H, m), 1.84 (3H,s), 2.80 (3H×2/3, s), 3.02 (3H×1/3, s), 2.97-3.11 (3H, m), 3.22-3.33(1H, m), 4.24 (1H×1/3, d, J=15 Hz), 4.45 (1H×2/3, d, J=15 Hz), 4.62(1H×1/3, d, J=15 Hz), 4.85 (1H×2/3, d, J=15 Hz), 5.39 (2H, m), 6.31 (1H,m), 6.99-7.15 (8H, m), 7.17-7.32 (5H, m), 7.47 (1H, d, J=8 Hz), 7.67(1H, d, J=8 Hz), 8.94 (1H, t, J=8 Hz)

EXAMPLE 34

The following object compounds were obtained according to a similarmanner to that of Example 33.

(1) MASS (m/z): 541 (M⁺ +1); NMR (CDCl₃, δ): 2.02 (3H, s), 2.74 (3H×2/3,s), 3.00 (3H×1/3, s), 3.06 (2H, m), 4.12 (1H×1/3, d, J=15 Hz), 4.37 (1H,m), 4.47 (1H×2/3, d, J=15 Hz), 4.57 (1H×1/3, d, J=15 Hz), 4.65 (1H, dd,J=4, 12 Hz), 4.88 (1H×2/3, d, J=15 Hz), 5.37 (1H, m), 5.70 (1H, m),6.96-7.20 (10H, m), 7.25-7.32 (4H, m), 7.49 (1H, d, J=8 Hz), 7.70 (1H,dd, J=2, 8 Hz), 9.00 (1H, d, J=8 Hz)

(2) MASS (m/z): 630 (M⁺ +1); NMR (CDCl₃, δ): 1.57-2.10 (4H, m), 2.79(3H×2/3, s), 2.97 (3H×1/3, s), 2.94-3.07 (2H, m), 3.42-3.49 (2H, m),4.27 (1H×1/3, d, J=15 Hz), 4.38 (1H×2/3, d, J=15 Hz), 4.43 (1H×1/3, d,J=15 Hz), 4.85 (1H×2/3, d, J=15 Hz), 5.35-5.62 (2H, m), 6.96-7.15 (9H,m), 7.17-7.33 (7H, m), 7.35-7.48 (3H, m), 7.56-7.82 (3H, m), 9.02 (1H,t, J=8 Hz)

(3) MASS: 568 (M⁺ +1); NMR (CDCl₃, δ): 1.61-1.71 (2H, m), 1.77-1.98 (2H,m), 1.90 (3H×2/3, s), 1.92 (3H×1/3, s), 2.81 (3H×2/3, s), 3.02 (3H×1/3,s), 2.95-3.05 (2H, m), 3.12-3.33 (2H, m), 4.26 (1H×1/3, d, J=15 Hz),4.44 (1H×1/3, d, J=15 Hz), 4.46 (1H×2/3, d, J=15 Hz), 4.88 (1H×2/3, d,J=15 Hz), 5.34-5.52 (2H, m), 6.60 (1H, m), 6.99-7.15 (9H, m), 7.22-7.32(5H, m), 7.46 (1H, d, J=8 Hz), 7.67 (1H, dd, J=2, 8 Hz), 9.01 (1H, t,J=8 Hz)

(4) MASS (m/z): 644 (M⁺ +1); NMR (CDCl₃, δ): 1.33-2.01 (6H, m), 2.77(3H×2/3, s), 3.00 (3H×1/3, s), 2.98-3.07 (2H, m), 3.21-3.48 (2H, m),4.26 (1H×1/3, d, J=15 Hz), 4.40 (1H×2/3, d, J=15 Hz), 4.62 (1H×1/3, d,J=15 Hz), 4.86 (1H×2/3, d, J=15 Hz), 5.42 (2H, m), 6.95-7.14 (8H, m),7.18-7.37 (8H, m), 7.47 (1H, d, J=8 Hz), 7.64-7.77 (3H, m), 8.97 (1H, m)

EXAMPLE 35

To a solution of Starting Compound (243 mg) inN,N-dimethylformamide-pyridine (4:1, 5 ml) was added sulfurtrioxide-pyridine complex (790 mg) at room temperature. The mixture wasstirred at the temperature for 12 hours and the solvent was evaporated.To this residue was added 10% aqueous ammonia with ice-cooling, and themixture was stirred for 30 minutes. The mixture was extracted threetimes with butanol, and the organic layer was washed with water. Thesolvent was evaporated, and the residue was redissolved in toluene, thenevaporated to give a solid. The product was purified by columnchromatography (silica gel, chloroform-methanol) to give Object Compound(191 mg) as white powders.

MASS (m/z): 499 (M-SO₃ +H⁺); NMR (CDCl₃, δ): 2.20-3.05 (5H, m),3.70-5.50 (6H, m), 6.55-7.65 (17H, m), 8.50-8.75 (1H, m)

EXAMPLE 36

The following object compound was obtained by treating Starting Compoundwith trifluoroacetic acid according to a similar manner to that ofPreparation 3, 4, 8 or 41.

MASS (m/z): 569 (M⁺ +1); NMR (CDCl₃, δ): 1.67 (2H, m), 1.98 (2H, m),2.55 (3H×1/2, s), 2.58 (3H×1/2, s), 2.68-2.78 (2H, m), 2.97 (1H, m),3.31 (1H, m), 3.68 (2H×1/2, s), 4.27-4.53 (2H×1/2, m), 4.99 (2H, m),6.93-7.70 (17H, m)

EXAMPLE 37

The following object compounds were obtained according to a similarmanner to that of Example 1 or 24.

(1) MASS: 647 (M+1); NMR (CDCl₃, δ): 2.52-2.72 (1H, m), 2.69 (3×2/3H,s), 2.80 (3×1/3H, s), 3.10-3.33 (3H, m), 3.37-3.52 (2H, m), 3.53-3.80(6H, m), 4.21 (2×1/3H, d, J=15 Hz), 4.23 (2×1/6H, d, J=16 Hz), 4.37(2×1/6H, d, J=16 Hz), 4.69 (2×1/3H, d, J=15 Hz), 5.02-5.30 (2H, m), 6.88(2×1/3H, d, J=8 Hz), 6.93 (2×2/3H, d, J=8 Hz), 7.03-7.21 (3H, m),7.22-7.33 (3H, m), 7.34-7.57 (4H, m), 7.58-7.83 (6H, m), 8.20 (1H, t,J=7 Hz)

(2) MASS: 646 (M+1); NMR (CDCl₃, δ): 2.52-2.77 (1H, m), 2.68 (3×2/3H,s), 2.83 (3×1/3H, s), 3.03-3.30 (3H, m), 3.30-3.48 (2H, m), 3.49-3.72(6H, m), 4.15 (2×1/3H, d, J=15 Hz), 4.30 (2×1/6H, d, J=16 Hz), 4.38(2×1/6H, d, J=16 Hz), 4.73 (2×1/3H, d, J=15 Hz), 5.13-5.38 (2H, m),6.80-7.00 (3H, m), 7.01-7.30 (6H, m), 7.30-7.48 (3H, m), 7.50-7.80 (5H,m), 7.94-8.20 (2H, m)

(3) MASS: 610 (M+1); NMR (CDCl₃, δ): 2.50-2.72 (1H, m), 2.73-3.08 (2H,m), 2.81 (3×2/3H, s), 2.87 (3×1/3H, s), 3.09-3.30 (1H, m), 3.19 (3×1/3H,s), 3.20 (3×2/3H, s), 3.31-3.70 (8H, m), 4.23 (2×1/6H, d, J=16 Hz), 4.50(2×1/3H, d, J=15 Hz), 4.65 (2×1/3H, d, J=15 Hz), 4.78 (2×1/6H, d, J=16Hz), 5.37-5.50 (1×1/3H, m), 5.51-5.60 (1×2/3H, m), 5.70-5.87 (1H, m),6.61 (1×2/3H, d, J=8 Hz), 6.78 (1H, s), 6.88 (1×1/3H, d, J=8 Hz),6.91-7.33 (12H, m), 7.38-7.50 (1H, m), 7.60-7.72 (1H, m), 9.87 (1H, s)

(4) MASS: 611 (M+1); NMR (CDCl₃, δ): 2.51-2.70 (1H, m), 2.81 (3×2/3H,s), 2.89 (3×1/3H, s), 2.94-3.09 (2H, m), 3.13 (1H, t, J=8 Hz), 3.22 (3H,s), 3.30-3.42 (2H, m), 3.43-3.70 (6H, m), 4.21 (2×1/6H, d, J=16 Hz),4.51 (2×1/3H, d, J=15 Hz), 4.67 (2×1/3H, d, J=15 Hz), 4.73 (2×1/6H, d,J=16 Hz), 5.34-5.58 (1H, m), 5.73 (1H, q, J=5 Hz), 6.54 (1×2/3H, d, J=8Hz), 6.67 (1×1/3H, d, J=8 Hz), 6.80-6.93 (1H, m), 6.98-7.09 (2H, m),7.11 (1H, d, J=8 Hz), 7.13-7.39 (7H, m), 7.40-7.60 (3H, m), 7.62-7.78(1H, m)

(5) MASS: 626 (M+1); NMR (CDCl₃, δ): 2.58-2.80 (1H, m), 2.67 (3×2/3H,s), 2.83 (3×1/3H, s), 2.89-3.02 (2H, m), 3.10-3.22 (1H, m), 3.30-3.48(2H, m), 3.49-3.72 (6H, m), 3.58 (3H, s), 4.22 (2×1/3H, d, J=15 Hz),4.31 (2×1/6H, d, J=16 Hz), 4.40 (2×1/6H, d, J=16 Hz), 4.75 (2×1/3H, d,J=15 Hz), 5.09-5.20 (1H, m), 5.21-5.34 (1H, m), 6.61 (2H, t, J=8 Hz),6.90-7.02 (3H, m), 7.03-7.14 (2H, m), 7.18-7.32 (5H, m), 7.42 (1H, d,J=8 Hz), 7.62 (1H, d, J=8 Hz), 8.02-8.20 (2H, m)

(6) MASS: 627 (M+1); NMR (CDCl₃, δ): 2.58-2.71 (1H, m), 2.68 (3×1/3H,s), 2.83 (3×2/3H, s), 2.88-3.08 (2H, m), 3.23-3.38 (1H, m), 3.40-3.60(2H, m), 3.61-3.80 (6H, m), 3.70 (3H, s), 4.23 (2×1/6H, d, J=16 Hz),4.29 (2×1/3H, d, J=15 Hz), 4.41 (2×1/6H, d, J=16 Hz), 4.69 (2×1/3H, d,J=15 Hz), 5.01-5.18 (2H, m), 6.69 (2×2/3H, d, J=15 Hz), 6.73 (2×1/3H, d,J=15 Hz), 6.97-7.14 (4H, m), 7.22-7.35 (5H, m), 7.43 (1H, t, J=8 Hz),7.50 (1H, s), 7.54-7.61 (1H, m), 7.62-7.71 (1H, m), 8.22 (1H, d, J=8 Hz)

(7) MASS: 569 (M+1); NMR (CDCl₃, δ): 2.51 (3H, s), 2.57 (3×3/4H, s),2.61-2.69 (1H, m), 2.73 (3×1/4H, s), 2.93 (6H, s), 2.99-3.12 (2H, m),3.27 (1H, dd, J=16, 5 Hz), 4.09 (2×1/6H, d, J=16 Hz), 4.27 (2×1/3H, d,J=15 Hz), 4.29 (2×1/6H, d, J=16 Hz), 4.51 (2×1/3H, d, J=15 Hz),5.09-5.22 (2H, m), 6.99-7.29 (10H, m), 7.46 (1H, d, J=8 Hz), 7.65 (1H,d, J=8 Hz), 7.99 (1×3/4H, d, J=8 Hz), 8.06 (1×1/4H, d, J=8 Hz),8.19-8.27 (2H, m)

(8) MASS: 570 (M+1); NMR (CDCl₃, δ): 2.52 (3H, s), 2.58 (3×2/3H, s),2.61-2.70 (1H, m), 2.73 (3×1/3H, s), 2.97 (3H, s), 3.00 (3H, s),2.98-3.08 (2H, m), 3.34 (1H, d, J=17 Hz), 4.02 (2×1/6H, d, J=16 Hz),4.27 (2×1/3H, d, J=15 Hz), 4.31 (2×1/6H, d, J=16 Hz), 4.57 (2×1/3H, d,J=15 Hz), 5.06-5.19 (2H, m), 7.07 (1H, d, J=8 Hz), 7.12-7.31 (7H, m),7.43 (1H, t, J=8 Hz), 7.51 (1H, s), 7.58 (1H, d, J=8 Hz), 7.68 (1H, d,J=8 Hz), 7.78 (1×1/4H, d, J=8 Hz), 7.80 (1×3/4H, d, J=8 Hz), 8.20(1×1/4H, s), 8.28 (1×3/4H, s), 8.32 (1H, d, J=8 Hz)

(9) MASS: 623 (M+1); NMR (CDCl₃, δ): 2.22 (3H, s), 2.26 (3H, s),2.25-2.42 (4H, m), 2.61 (3×2/3H, s), 2.68-2.78 (1H, m), 2.82 (3×1/3H,s), 2.95-3.10 (2H, m), 3.19-3.30 (1H, m), 3.35-3.50 (2H, m), 3.55-3.70(2H, m), 4.18 (2×1/6H, d, J=16 Hz), 4.20 (2×1/3H, d, J=15 Hz), 4.32(2×1/6H, d, J=16 Hz), 4.68 (2×1/3H, d, J=15 Hz), 5.12-5.30 (2H, m),6.76-7.18 (11H, m), 7.23 (1H, t, J=8 Hz), 7.44 (1H, d, J=8 Hz), 7.65(1H, d, J=8 Hz), 7.99-8.10 (2H, m)

(10) MASS: 624 (M+1); NMR (CDCl₃, δ): 2.29 (3H, s), 2.31 (3H, s),2.34-2.53 (4H, m), 2.59 (3×2/3H, s), 2.63-2.72 (1H, m), 2.81 (3×1/3H,s), 3.00-3.10 (2H, m), 3.28-3.39 (1H, m), 3.42-3.58 (2H, m), 3.63-3.72(2H, m), 4.09 (2×1/6H, d, J=16 Hz), 4.32 (2×1/6H, d, J=16 Hz), 4.27(2×1/3H, d, J=15 Hz), 4.60 (2×1/3H, d, J=15 Hz), 5.02-5.16 (2H, m),6.74-7.06 (3H, m), 7.11-7.22 (6H, m), 7.29 (1H, t, J=8 Hz), 7.43 (1H, t,J=8 Hz), 7.50 (1H, s), 7.58 (1H, d, J=8 Hz), 7.68 (2×2/3H, d, J=8 Hz),7.72 (2×1/3H, d, J=8 Hz), 8.22 (1H, d, J=8 Hz)

(11) MASS: 623 (M+1); NMR (CDCl₃, δ): 2.13 (3×1/3H, s), 2.16 (3×2/3H,s), 2.23 (3H, s), 2.28-2.42 (4H, m), 2.61 (3×2/3H, s), 2.59-2.74 (1H,m), 2.82 (3×1/3H, s), 2.99-3.09 (2H, m), 3.21 (1H, t, J=15 Hz),3.36-3.48 (2H, m), 3.52-3.71 (2H, m), 4.12 (2×1/6H, d, J=16 Hz), 4.21(2×1/6H, d, J=16 Hz), 4.40 (2×1/3H, d, J=15 Hz), 4.58 (2×1/3H, d, J=15Hz), 4.98-5.28 (2H, m), 6.75 (1H, t, J=8 Hz), 6.98 (1H, d, J=8 Hz),7.02-7.20 (9H, m), 7.23 (1H, t, J=8 Hz), 7.41 (1H, d, J=8 Hz), 7.64 (1H,d, J=8 Hz), 7.96-8.09 (2H, m)

(12) MASS: 640 (M+1); NMR (CDCl₃, δ): 2.13 (3×1/3H, s), 2.14 (3×2/3H,s), 2.23 (3H, s), 2.31-2.50 (4H, m), 2.59 (1H, dd, J=17, 8 Hz), 2.63(3×2/3H, s), 2.85 (3×1/3H, s), 3.01-3.15 (2H, m), 3.21-3.35 (1H, m),3.40-3.58 (2H, m), 3.60-3.74 (2H, m), 4.10 (2×1/6H, d, J=16 Hz), 4.24(2×1/6H, d, J=16 Hz), 4.47 (2×1/3H, d, J=15 Hz), 4.53 (2×1/3H, d, J=15Hz), 4.89-5.20 (2H, m), 6.80 (1H, t, J=8 Hz), 7.07-7.30 (8H, m),7.38-7.47 (2H, m), 7.63-7.90 (4H, m), 8.11 (1H, t, J=8 Hz)

(13) MASS: 623 (M+1); NMR (CDCl₃, δ): 2.13 (3×1/3H, s), 2.15 (3×2/3H,s), 2.29 (3H, s), 2.33-2.49 (4H, m), 2.52-2.70 (1H, m), 2.62 (3×2/3H,s), 2.83 (3×1/3H, s), 2.99-3.17 (2H, m), 3.30 (1H, t, J=15 Hz),3.41-3.58 (2H, m), 3.60-3.72 (2H, m), 4.06 (2×1/6H, d, J=16 Hz), 4.22(2×1/6H, d, J=16 Hz), 4.48 (2×1/3H, d, J=15 Hz), 4.52 (2×1/3H, d, J=15Hz), 4.93-5.22 (2H, m), 6.73 (1×1/3H, d, J=8 Hz), 6.79 (1×2/3H, d, J=8Hz), 7.07-7.31 (9H, m), 7.42 (1H, s), 7.49 (1H, s), 7.57 (1H, d, J=8Hz), 7.61-7.73 (2H, m), 8.20 (1H, d, J=8 Hz)

(14) MASS: 598 (M+1); NMR (CDCl₃, δ): 2.60-2.73 (1H, m), 2.82 (3×3/4H,s), 2.88 (3×1/4H, s), 2.92-3.12 (2H, m), 3.14-3.26 (1H, m), 3.30-3.45(2H, m), 3.50-3.70 (6H, m), 4.30 (2×1/6H, d, J=17 Hz), 4.42 (2×1/3H, d,J=15 Hz), 4.50 (2×1/6H, d, J=17 Hz), 4.60 (2×1/3H, d, J=15 Hz),4.98-5.08 (2×1/6H, m), 5.14-5.26 (2×5/6H, m), 6.82 (1×1/4H, d, J=5 Hz),6.86 (1×3/4H, d, J=5 Hz), 6.98 (1H, s), 7.05-7.18 (6H, m), 7.27 (1H, t,J=8 Hz), 7.40 (1H, d, J=8 Hz), 7.63 (1H, d, J=5 Hz), 8.00-8.10 (2H, m),8.53 (1H, d, J=5 Hz), 9.09 (1×3/4H, s), 9.10 (1×1/4H, s)

(15) MASS: 599 (M+1); NMR (CDCl₃, δ): 2.60-2.70 (1H, m), 2.82 (3×3/4H,s), 2.87 (3×1/4H, s), 2.98-3.18 (2H, m), 3.27-3.33 (1H, m), 3.40-3.57(2H, m), 3.62-3.78 (6H, m), 4.32 (2×1/6H, d, J=17 Hz), 4.45 (2×1/6H, d,J=17 Hz), 4.48 (2×1/3H, d, J=15 Hz), 4.60 (2×1/3H, d, J=15 Hz),4.93-5.22 (2H, m), 6.86 (1×1/4H, d, J=5 Hz), 6.93 (1×3/4H, d, J=5 Hz),7.15-7.23 (5H, m), 7.30 (1H, t, J=8 Hz), 7.43 (1H, t, J=8 Hz), 7.50 (1H,d, J=8 Hz), 7.58 (1H, d, J=8 Hz), 7.62-7.71 (2H, m), 8.18-8.22 (1H, m),8.57-8.62 (1H, m), 9.10 (1H, s)

(16) MASS: 648 (M+1); NMR (CDCl₃, δ): 2.60-2.78 (1H, m), 2.81 (3×4/5H,s), 2.92 (3×1/5H, s), 2.97-3.22 (3H, m), 3.28-3.42 (2H, m), 3.48-3.65(6H, m), 4.67 (2×1/2H, d, J=15 Hz), 4.89 (2×1/2H, d, J=15 Hz), 5.11-5.32(2H, m), 6.91-7.12 (7H, m), 7.20 (1H, t, J=8 Hz), 7.41 (1H, d, J=8 Hz),7.61 (1H, d, J=8 Hz), 7.70-7.78 (2H, m), 7.94-8.02 (1H, m), 8.03-8.27(3H, m), 8.70 (1×1/5H, s), 8.73 (1×4/5H, s)

(17) MASS: 649 (M+1); NMR (CDCl₃, δ): 2.58-2.73 (1H, m), 2.82 (3×3/4H,s), 2.93 (3×1/4H, s), 3.02-3.32 (3H, m), 3.40-3.55 (2H, m), 3.58-3.77(6H, m), 4.59 (2×1/6H, d, J=16 Hz), 4.68 (2×1/6H, d, J=16 Hz), 4.70(2×1/3H, d, J=15 Hz), 4.90 (2×1/3H, d, J=15 Hz), 5.03-5.28 (2H, m),7.02-7.22 (5H, m), 7.29 (1H, t, J=8 Hz), 7.41 (1H, t, J=8 Hz), 7.48 (1H,s), 7.56 (1H, d, J=8 Hz), 7.68 (1H, d, J=8 Hz), 7.70-7.82 (3H, m),7.98-8.03 (1H, m), 8.07-8.14 (1H, m), 8.19 (1H, d, J=8 Hz), 8.70(1×1/4H, s), 8.75 (1×3/4H, s)

(18) MASS: 647 (M+1); NMR (CDCl₃, δ): 2.60-2.77 (1H, m), 2.82 (3×3/4H,s), 2.93 (3×1/4H, s), 3.00-3.25 (3H, m), 3.30-3.45 (2H, m), 3.50-3.70(6H, m), 4.62 (2×1/3H, s), 4.67 (2×1/3H, d, J=15 Hz), 4.92 (2×1/3H, d,J=15 Hz), 5.19-5.31 (2H, m), 6.95-7.30 (9H, m), 7.41 (1H, d, J=8 Hz),7.52 (1H, t, J=8 Hz), 7.61-7.71 (2H, m), 7.79 (1H, d, J=8 Hz), 7.98-8.18(4H, m)

(19) MASS: 648 (M+1); NMR (CDCl₃, δ): 2.59-2.71 (1H, m), 2.74 (3×3/4H,s), 2.89 (3×1/4H, s), 3.01-3.20 (2H, m), 3.21-3.33 (1H, m), 3.40-3.55(2H, m), 3.60-3.80 (6H, m), 4.60 (2×1/6H, d, J=16 Hz), 4.63 (2×1/6H, d,J=16 Hz), 4.68 (2×1/3H, d, J=15 Hz), 4.89 (2×1/3H, d, J=15 Hz),5.05-5.25 (2H, m), 7.11-7.32 (7H, m), 7.41-7.59 (4H, m), 7.67-7.82 (4H,m), 8.00-8.12 (2H, m), 8.23 (1H, d, J=8 Hz)

(20) MASS: 647 (M+1); NMR (CDCl₃, δ): 2.63-2.80 (1H, m), 2.71 (3×3/4H,s), 2.89 (3×1/4H, s), 2.99-3.30 (3H, m), 3.31-3.49 (2H, m), 3.50-3.70(6H, m), 4.30 (2×1/6H, d, J=16 Hz), 4.58 (2×1/6H, d, J=16 Hz), 4.69(2×2/3H, s), 5.12-5.30 (2H, m), 6.95-7.20 (7H, m), 7.21-7.30 (2H, m),7.33-7.49 (2H, m), 7.60-7.77 (2H, m), 7.80 (1×1/4H, s), 7.88 (1×3/4H,s), 8.05-8.20 (3H, m), 8.90 (1H, d, J=2 Hz)

(21) MASS: 648 (M+1); NMR (CDCl₃, δ): 2.61-2.75 (1H, m), 2.70 (3×3/4H,s), 2.86 (3×1/4H, s), 3.00-3.18 (2H, m), 3.22-3.33 (1H, m), 3.40-3.58(2H, m), 3.60-3.80 (6H, m), 4.19 (2×1/6H, d, J=16 Hz), 4.58 (2×1/6H, d,J=16 Hz), 4.70 (2×1/3H, d, J=15 Hz), 4.81 (2×1/3H, d, J=15 Hz),5.03-5.22 (2H, m), 7.10-7.60 (11H, m), 7.68 (1H, d, J=8 Hz), 7.71-7.82(2H, m), 7.83 (1H, s), 8.12 (1H, d, J=8 Hz), 8.21 (1H, t, J=8 Hz), 8.89(1H, d, J=2 Hz)

(22) MASS: 598 (M+1); NMR (CDCl₃, δ): 2.63-2.75 (1H, m), 2.80 (3×3/4H,s), 2.88 (3×1/4H, s), 2.94-3.20 (3H, m), 3.30-3.45 (2H, m), 3.50-3.67(6H, m), 4.39 (2×1/6H, d, J=17 Hz), 4.48 (2×1/6H, d, J=17 Hz), 4.49(2×1/3H, d, J=15 Hz), 4.70 (2×1/3H, d, J=15 Hz), 5.10-5.23 (2H, m),6.93-6.98 (1H, m), 7.03-7.13 (6H, m), 7.22-7.28 (1H, m), 7.42 (1H, d,J=8 Hz), 7.62 (1H, d, J=8 Hz), 8.02-8.17 (2H, m), 8.33-8.49 (3H, m)

(23) MASS: 599 (M+1); NMR (CDCl₃, δ): 2.58-2.70 (1H, m), 2.81 (3×5/6H,s), 2.86 (3×1/6H, s), 3.00-3.18 (2H, m), 3.20-3.31 (1H, m), 3.39-3.54(2H, m), 3.60-3.75 (6H, m), 4.41 (2×1/3H, s), 4.48 (2×1/3H, d, J=15 Hz),4.70 (2×1/3H, d, J=15 Hz), 5.02-5.19 (2H, m), 7.10-7.22 (6H, m), 7.29(1H, t, J=8 Hz), 7.42 (1H, t, J=8 Hz), 7.50 (1H, s), 7.56 (1H, d, J=8Hz), 7.63-7.78 (2H, m), 8.13-8.22 (1H, m), 8.33-8.50 (2H, m)

(24) MASS: 675 (M+1); NMR (CDCl₃, δ): 2.61-2.74 (1H, m), 2.71 (3×3/4H,s), 2.81 (3×1/4H, s), 3.00-3.20 (2H, m), 3.28-3.38 (1H, m), 3.41-3.58(2H, m), 3.62-3.80 (6H, m), 4.15 (2×1/6H, d, J=16 Hz), 4.41 (2×1/6H, d,J=16 Hz), 4.42 (2×1/3H, d, J=15 Hz), 4.60 (2×1/3H, d, J=15 Hz),5.09-5.20 (2H, m), 7.12-7.80 (14H, m), 8.22 (1H, d, J=8 Hz), 8.30 (1H,d, J=8 Hz), 8.41 (1×1/4H, s), 8.50 (1×3/4H, s), 8.60-8.70 (1H, m),9.12-9.22 (1H, m)

(25) MASS: 674 (M+1); NMR (CDCl₃, δ): 2.64-2.78 (1H, m), 2.65 (3×3/4H,s), 2.79 (3×1/4H, s), 2.98-3.27 (3H, m), 3.29-3.45 (2H, m), 3.48-3.70(6H, m), 4.16 (2×1/6H, d, J=16 Hz), 4.33 (2×1/3H, d, J=15 Hz), 4.37(2×1/6H, d, J=16 Hz), 4.57 (2×1/3H, d, J=15 Hz), 5.09-5.30 (2H, m), 6.99(1H, s), 7.06-7.19 (6H, m), 7.20-7.30 (1H, m), 7.33-7.48 (3H, m),7.53-7.68 (2H, m), 8.09-8.28 (3H, m), 8.40 (1×1/4H, s), 8.48 (1×3/4H,s), 8.63 (1H, s), 9.17 (1H, s)

(26) MASS: 674 (M+1); NMR (CDCl₃, δ): 2.61-2.78 (1H, m), 2.64 (3×3/4H,s), 2.80 (3×1/4H, s), 2.98-3.12 (2H, m), 3.13-3.25 (1H, m), 3.30-3.48(2H, m), 3.52-3.68 (6H, m), 4.18 (2×1/6H, d, J=16 Hz), 4.33 (2×1/3H, d,J=15 Hz), 4.40 (2×1/6H, d, J=16 Hz), 4.65 (2×1/3H, d, J=15 Hz),5.11-5.30 (2H, m), 6.98-7.02 (1H, m), 7.08-7.20 (6H, m), 7.22-7.32 (2H,m), 7.43 (2H, t, J=8 Hz), 7.63 (1H, d, J=8 Hz), 7.80 (1H, t, J=8 Hz),8.02-8.20 (2H, m), 8.30 (1H, t, J=8 Hz), 8.38 (1H, d, J=8 Hz), 8.47 (1H,s), 8.68 (1H, d, J=5 Hz)

(27) MASS: 675 (M+1); NMR (CDCl₃, δ): 2.61-2.72 (1H, m), 2.69 (3×3/4H,s), 2.81 (3×1/4H, s), 3.01-3.18 (2H, m), 3.25-3.35 (1H, m), 3.40-3.58(2H, m), 3.62-3.79 (6H, m), 4.19 (2×1/6H, d, J=16 Hz), 4.38 (2×1/3H, d,J=15 Hz), 4.42 (2×1/6H, d, J=16 Hz), 4.69 (2×1/3H, d, J=15 Hz),5.10-5.22 (2H, m), 7.12-7.27 (6H, m), 7.31 (2H, t, J=8 Hz), 7.43 (1H, t,J=8 Hz), 7.50-7.60 (2H, m), 7.67-7.85 (3H, m), 8.21 (1H, d, J=8 Hz),8.27-8.40 (2H, m), 8.48 (1H, s), 8.68 (1H, d, J=5 Hz)

(28) MASS (m/z): 548 (M⁺ +1); NMR (CDCl₃, δ): 0.88-0.98 (6H, m), 2.10(1H, m), 2.71 (1H, dd, J=6, 15 Hz), 2.91 (3H×1/4, s), 3.03 (3H×3/4, s),3.22 (1H, dd, J=4, 15 Hz), 3.38 (2H, m), 3.60 (6H, m), 4.33 (1H×3/4, d,J=15 Hz), 4.64 (2H×1/4, s), 4.87 (1H×3/4, d, J=15 Hz), 4.87 (1H, m),5.33 (1H, m), 7.02 (1H, s), 7.12 (1H, t, J=8 Hz), 7.22-7.37 (6H, m),7.43 (1H, d, J=8 Hz), 7.64 (1H, d, J=8 Hz), 7.97 (1H×1/4, d, J=7 Hz),8.07 (1H×3/4, d, J=7 Hz), 8.18 (1H, d, J=7 Hz)

(29) MASS (m/z): 549 (M⁺ +1); NMR (CDCl₃, δ): 0.91-0.99 (6H, m), 2.08(1H, m), 2.66 (1H, m), 2.88 (3H×1/4, s), 3.02 (3H×3/4, s), 3.32 (1H, dd,J=3, 16 Hz), 3.47 (2H, m), 3.67 (6H, m), 4.35 (1H×3/4, d, J=15 Hz), 4.56(1H×1/4, d, J=16 Hz), 4.69 (1H×1/4, d, J=16 Hz), 4.79 (1H×3/4, d, J=15Hz), 4.81 (1H, m), 5.15 (1H, m), 7.18-7.37 (6H, m), 7.42 (1H, t, J=8Hz), 7.50 (1H, s), 7.54 (1H, d, J=8 Hz), 7.65 (2H, d, J=8 Hz), 8.31 (1H,m)

(30) MASS (m/z): 602 (M⁺ +1); NMR (CDCl₃, δ): 0.62-1.21 (5H, m),1.37-1.89 (8H, m), 2.62-2.71 (1H, m), 2.88 (3H×1/3, s), 2.89 (3H×2/3,s), 3.27 (1H, dd, J=4, 15 Hz), 3.41 (2H, m), 3.62 (6H, m), 4.14 (1H×2/3,d, J=15 Hz), 4.54 (1H×1/3, d, J=16 Hz), 4.64 (1H×1/3, d, J=16 Hz), 4.80(1H×2/3, d, J=15 Hz), 5.02 (1H, m), 5.19 (1H×1/3, m), 5.27 (1H×2/3, m),6.90 (1H, s), 7.10-7.38 (7H, m), 7.45 (1H, d, J=8 Hz), 7.65 (1H, d, J=8Hz), 7.77 (1H×1/3, d, J=7 Hz), 7.95 (1H×2/3, d, J=7 Hz), 8.08 (1H, t,J=7 Hz)

(31) MASS (m/z): 603 (M⁺ +1); NMR (CDCl₃, δ): 0.62-1.25 (5H, m),1.35-1.76 (8H, m), 2.62-2.72 (1H, m), 2.91 (3H×1/3, s), 2.99 (3H×2/3,s), 3.28 (1H, dd, J=3.15 Hz), 3.48 (2H, m), 3.68 (6H, m), 4.37 (1H×2/3,d, J=15 Hz), 4.62 (2H×1/3, s), 4.77 (1H×2/3, d, J=15 Hz), 5.02 (1H, m),5.15 (1H, m), 7.18-7.38 (5H, m), 7.43 (1H t, J=8 Hz), 7.52 (1H, m), 7.55(1H, d, J=8 Hz), 7.67 (2H, d, J=8 Hz), 8.23 (1H, m)

(32) MASS (m/z): 695 (M⁺ +1); NMR (CDCl₃, δ): 2.34 (3H, s), 2.57 (4H,m), 2.58 (3H×2/3, s), 2.65 (1H, dd, J=7, 16 Hz), 2.78 (3H×1/3, s), 3.03(2H, m), 3.20 (4H, m), 3.30 (1H, m), 3.47 (2H, m), 3.68 (6H, m), 4.01(1H×1/3, d, J=16 Hz), 4.21 (1H×2/3, d, J=15 Hz), 4.30 (1H×1/3, d, J=16Hz), 4.54 (1H×2/3, d, J=15 Hz), 5.10 (2H, m), 6.83-7.02 (4H, m), 7.17(5H, m), 7.32 (1H, d, J=8 Hz), 7.44 (1H, t, J=8 Hz), 7.51 (1H, s), 7.57(1H, d, J=8 Hz), 7.64-7.71 (2H, m), 8.21 (1H, d, J=8 Hz)

(33) MASS (m/z): 694 (M³⁰ +1); NMR (CDCl₃, δ): 2.34 (3H, s), 2.57 (4H,m), 2.60 (3H×2/3, s), 2.72 (1H, m), 2.82 (3H×1/3, s), 3.02 (2H, d, J=7Hz), 3.17 (5H, m), 3.37 (2H, m), 3.58 (6H, m), 4.07 (1H×1/3, d, J=16Hz), 4.17 (1H×2/3, d, J=15 Hz), 4.30 (1H×1/3, d, J=16 Hz), 4.63 (1H×2/3,d, J=15 Hz), 5.14 (1H, q, J=7 Hz), 5.22-5.33 (1H, m), 6.81 (2H, d, J=8Hz), 6.90 (1H, d, J=8 Hz), 6.98 (2H, d, J=8 Hz), 7.07 (6H, m), 7.22-7.27(1H, m), 7.44 (1H, d, J=8 Hz), 7.64 (1H, d, J=8 Hz), 8.05 (1H, t, J=7Hz), 8.14-8.21 (1H, m)

(34) MASS (m/z): 597 (M⁺ +1); NMR (CDCl₃, δ): 2.59-2.72 (1H, m), 2.73(3H×2/3, s), 2.88 (3H×1/3, s), 2.91-3.06 (2H, m), 3.16 (1H, dt, J=4, 16Hz), 3.35 (2H, m), 3.58 (6H, m), 4.12 (1H×2/3, d, J=15 Hz), 4.37(1H×1/3, d, J=16 Hz), 4.53 (1H×1/3, d, J=16 Hz), 4.73 (1H×2/3, d, J=15Hz), 5.14-5.27 (2H, m), 6.94-7.15 (8H, m), 7.27-7.29 (3H, m), 7.44 (1H,d, J=8 Hz), 7.65 (1H, d, J=8 Hz), 8.05-8.14 (2H, m), 8.32 (1H, d, J=5Hz)

(35) MASS (m/z): 598 (M ⁺ +1); NMR (CDCl₃, δ): 2.54-2.69 (1H, m), 2.77(3H×2/3, s), 2.89 (3H×1/3, s), 2.91-3.12 (2H, m), 3.27 (1H, dt, J=4, 16Hz), 3.47 (2H, m), 3.67 (6H, m), 4.24 (1H×2/3, d, J=15 Hz), 4.42(1H×1/3, d, J=16 Hz), 4.49 (1H×1/3, d, J=16 Hz), 4.71 (1H×2/3, d, J=15Hz), 5.03 (1H×1/3, m), 5.11 (1H×2/3, m), 5.15 (1H, m), 7.00-7.13 (5H,m), 7.27-7.32 (3H, m), 7.45 (1H, t, J=8 Hz), 7.52 (1H, s), 7.58 (1H, d,J=8 Hz), 7.64-7.72 (2H, m), 8.21 (1H, d, J=8 Hz), 8.39 (2H, d, J=5 Hz)

(36) MASS (m/z): 664 (M⁺ +1); NMR (CDCl₃, δ): 2.61-2.70 (1H, m), 2.67(3H×3/4,s), 2.81 (3H×1/4, s), 3.07 (2H, m), 3.27-3.37 (1H, m), 3.48 (2H,m), 3.68 (6H, m), 4.18 (1H×1/4, d, J=16 Hz), 4.38 (1H×1/4, d, J=16 Hz),4.39 (1H×3/4, d, J=15 Hz), 4.62 (1H×3/4, d, J=15 Hz), 5.13 (2H, m),7.06-7.22 (7H, m), 7.31 (1H, t, J=8 Hz), 7.44 (1H, t, J=8 Hz), 7.52 (1H,s), 7.55-7.59 (3H, m), 7.70 (2H, t, J=8 Hz), 8.11 (1H, s), 8.21 (1H, m),8.53 (1H×3/4, s), 8.55 (1H×1/4, s)

(37) MASS (m/z): 663 (M⁺ +1); NMR (CDCl₃, δ): 2.67 (3H×3/4, s), 2.73(1H, dd, J=7, 16 Hz), 2.80 (3H×1/4, s), 3.04 (2H, m), 3.22 (1H, dd, J=3,16 Hz), 3.37 (2H, m), 3.60 (6H, m), 4.18 (1H×1/4, d, J=16 Hz), 4.33(1H×3/4, d, J=15 Hz), 4.35 (1H×1/4, d, J=15 Hz), 4.61 (1H×3/4, d, J=16Hz), 5.18 (1H, q, J=7 Hz), 5.27 (1H, m), 6.99-7.15 (10H, m), 7.23 (1H,d, J=8 Hz), 7.44 (1H, d, J=8 Hz), 7.51 (2H, m), 7.63 (1H, d, J=8 Hz),8.10 (1H, s), 8.13 (2H, m), 8.50 (1H×3/4, s), 8.53 (1H×1/4, s)

(38) MASS (m/z): 648 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.72 (1H, m), 2.68(3/4×3H, s), 2.85 (1/4×3H, s), 2.98-3.21 (2H, m), 3.21-3.38 (1H, m),3.38-3.79 (8H, m), 4.29 (1/4×1H, d, J=17 Hz), 4.56 (1/4×1H, d, J=17 Hz),4.65 (3/4×2H, ABq, Δ=0.22, J=15 Hz), 5.02-5.25 (2H, m), 7.00-8.28 (17H,m), 8.65 (1/4×1H, d, J=2 Hz), 8.73 (3/4×1H, d, J=2 Hz)

(39) MASS (m/z): 647 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.76 (1H, m), 2.71(3/4×3H, s), 2.85 (1/4×3H, s), 2.95-3.30 (3H, m), 3.35-3.75 (8H, m),4.30 (1/4×1H, d, J=17 Hz), 4.57 (1/4×1H, d, J=17 Hz), 4.63 (3/4×2H, ABq,Δ=0.12, J=15 Hz), 5.05-5.28 (2H, m), 6.95-8.15 (17H, m), 8.65 (1/4×1H,d, J=2 Hz), 8.73 (3/4×1H, d, J=2 Hz), 9.75 (1/4×1H, s), 9.95 (3/4×1H, s)

(40) MASS (m/z): 648 (M+H)⁺ ; NMR (CDCl₃, δ): 2.54-2.73 (1H, m), 2.70(2/3×3H, s), 2.87 (1/3×3H, s), 2.95-3.18 (2H, m), 3.20-3.78 (9H, m),4.43 (1/3×2H, ABq, Δ=0.16, J=17 Hz), 4.51 (2/3×1H, d, J=15 Hz), 4.80(2/3×1H, d, J=15 Hz), 5.00-5.22 (2H, m), 7.08-7.80 (14H, m), 7.95-8.30(3H, m), 8.90 (1H, d, J=2 Hz)

(41) MASS (m/z): 647 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.75 (1H, m), 2.70(2/3×3H, s), 2.87 (1/3×3H, s), 2.95-3.14 (2H, m), 3.14-3.33 (1H, m),3.33-3.75 (8H, m), 4.46 (1/3×2H, ABq, Δ=0.15, J=17 Hz), 4.48 (2/3×1H, d,J=15 Hz), 4.82 (2/3×1H, d, J=15 Hz), 5.08-5.25 (2H, m), 6.94-7.72 (13H,m), 7.82-8.14 (4H, m), 8.89 (1H, d, J=2 Hz), 9.70 (1/3×1H, s), 9.72(2/3×1H, s)

(42) MASS (m/z): 655 (M+H)⁺ ; NMR (CDCl₃, δ): 2.20 (3H, s), 2.58-2.70(1H, m), 2.61 (3/4×3H, s), 2.72 (1/4×3H, s), 2.93-3.18 (2H, m),3.22-3.37 (1H, m), 3.37-3.80 (8H, m), 3.95 (1/4×1H, d, J=17 Hz), 4.24(3/4×1H, d, J=15 Hz), 4.29 (1/4×1H, d, J=17 Hz), 4.56 (3/4×1H, d, J=15Hz), 5.00-5.20 (2H, m), 7.06-7.80 (14H, m), 7.92-8.28 (2H, m)

(43) MASS (m/z): 654 (M+H)⁺ ; NMR (CDCl₃, δ): 2.20 (3H, s), 2.58-2.72(1H, m), 2.59 (3/4×3H, s), 2.71 (1/4×3H, s), 2.88-3.12 (2H, m),3.14-3.30 (1H, m), 3.33-3.78 (8H, m), 3.88 (1/4×1H, d, J=17 Hz), 4.29(1/4×1H, d, J=17 Hz), 4.39 (3/4×2H, ABq, Δ=0.10, J=15 Hz), 5.00-5.18(2H, m), 6.90-8.50 (16H, m), 9.84 (1/4×1H, s), 9.95 (3/4×1H, s)

(44) MASS: 624 (M+1); NMR (CDCl₃, δ): 2.05-2.20 (1H, m), 2.23-2.43 (4H,m), 2.25 (3H, s), 2.45-2.60 (2H, m), 2.70 (3×2/3H, s), 2.71-2.80 (1H,m), 2.87 (3×1/3H, s), 2.97-3.14 (2H, m), 3.40-3.53 (2H, m), 3.60-3.75(2H, m), 4.30 (2×1/4H, d, J=16 Hz), 4.35 (2×1/4H, d, J=15 Hz), 4.41(2×1/4H, d, J=16 Hz), 4.69 (2×1/4H, d, J=15 Hz), 4.61-4.72 (1H, m),5.10-5.20 (1H, m), 7.03-7.20 (8H, m), 7.23-7.34 (3H, m), 7.40-7.56 (3H,m), 7.67 (1H, d, J=8 Hz), 7.87-7.93 (1H, m), 8.17 (1H, t, J=8 Hz)

(45) MASS (m/z): 580 (M⁺ +1); NMR (CDCl₃, δ): 2.64-2.75 (1H, m), 2.86(1H, t, J=15 Hz), 3.23-3.43 (4H, m), 3.68 (6H, m), 4.59-4.74 (1H, m),4.80-4.87 (1H, m), 5.21-5.37 (2H, m), 6.84 (1H, m), 6.94-7.27 (11H, m),7.37-7.62 (2H, m), 8.05-8.31 (2H, m)

(46) MASS (m/z): 581 (M⁺ +1); NMR (CDCl₃, δ): 2.64-2.78 (1H, m),2.85-3.00 (1H, m), 3.31-3.59 (4H, m), 3.67 (6H, m), 4.57-4.75 (1H, m),4.84-4.92 (1H, m), 5.21 (1H, m), 5.39 (1H, d, J=16 Hz), 6.89 (1H, d, J=8Hz), 7.01 (1H, t, J=8 Hz), 7.12-7.31 (8H, m), 7.38-7.45 (1H, m),7.52-7.56 (2H, m), 7.67 (1H, d, J=8 Hz), 7.92-8.12 (1H, m), 8.24-8.41(1H, m)

(47) MASS (m/z): 603 (M+1)⁺ ; NMR (CDCl₃, δ): 2.61 (1H×1/3, dd, J=16.0,6.0 Hz), 2.67 (1H×2/3, dd, J=16.0, 6.0 Hz), 2.79 (3H×1/3, s), 2.87(3H×2/3, s), 3.16-3.57 (5H, m), 3.61-3.80 (6H, m), 4.37 (1H, d, J=14.5Hz), 4.49 (1H×1/3, d, J=14.5 Hz), 4.66 (1H×2/3, d, J=14.5 Hz), 5.03-5.21(2H, m), 6.81-6.90 (2H, m), 7.01-7.13 (3H, m), 7.23-7.36 (4H, m), 7.44(1H, t, J=7.5 Hz), 7.51 (1H, d, J=1.5 Hz), 7.55-7.74 (3H, m), 8.22 (1H,d, J=7.5 Hz)

(48) MASS (m/z): 602 (M+1)⁺ ; NMR (CDCl₃, δ): 2.60 (1H×1/3, dd, J=16.0,7.0 Hz), 2.67 (1H×2/3, dd, J=16.0, 7.0 Hz), 2.80 (3H×2/3, s), 2.88(3H×1/3, s), 3.12-3.38 (3H, m), 3.40-3.55 (2H, m), 3.59-3.74 (6H, m),4.35 (1H×2/3, d, J=14.5 Hz), 4.39 (1H×1/3, d, J=14.5 Hz), 4.49 (1H×1/3,d, J=14.5 Hz), 4.70 (1H×2/3, d, J=14.5 Hz), 5.04-5.21 (2H, m), 6.76-6.84(2H, m), 6.98-7.19 (5H, m), 7.23-7.34 (4H, m), 7.43 (1H, d, J=7.5 Hz),7.67 (1H, d, J=7.5 Hz), 7.81 (1H×1/3, d, J=7.5 Hz), 7.89 (1H×2/3, d,J=7.5 Hz), 8.07 (1H, d, J=7.5 Hz), 9.49 (1H×1/3, br s), 9.55 (1H×2/3, brs)

(49) MASS (m/z): 676 (M+H)⁺ ; NMR (CDCl₃, δ): 2.57-2.78 (1H, m), 2.62(2/3×3H, s), 2.83 (1/3×3H, s), 2.93-3.11 (2H, m), 3.11-3.29 (1H, m),3.29-3.72 (8H, m), 3.93 (3H, s), 4.27 (2/3×1H, d, J=15 Hz), 4.30(1/3×2H, ABq, Δ=0.20, J=17 Hz), 4.72 (2/3×1H, d, J=15 Hz), 5.09-5.32(2H, m), 6.50 (1H, m), 6.93-8.14 (17H, m), 10.00 (1H, br s)

(50) MASS (m/z): 677 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53-2.72 (1H, m), 2.62(2/3×3H, s), 2.82 (1/3×3H, s), 2.95-3.13 (2H, m), 3.21-3.38 (1H, m),3.38-3.88 (8H, m), 3.94 (3H, s), 4.28 (1/3×2H, ABq, Δ=0.21, J=17 Hz),4.29 (2/3×1H, d, J=15 Hz), 4.69 (2/3×1H, d, J=15 Hz), 5.02-5.22 (2H, m),6.51 (1H, d, J=2 Hz), 6.97-7.78 (17H, m), 8.15-8.27 (1H, m)

(51) MASS (m/z): 640 (M+H)⁺ ; NMR (CDCl₃, δ): 2.58 (2/3×3H, s),2.62-2.78 (1H, m), 2.73 (1/3×3H, s), 2.92-3.04 (2H, m), 3.05 (1/3×6H,s), 3.07 (2/3×6H, s), 3.13-3.30 (1H, m), 3.32-3.72 (8H, m), 3.82(1/3×1H, d, J=17 Hz), 4.28 (1/3×1H, d, J=17 Hz), 4.32 (2/3×2H, ABq,Δ=0.24, J=15 Hz), 5.02-5.33 (2H, m), 6.41 (1H, d, J=9 Hz), 6.95-8.15(14H, m), 10.00 (1H, br s)

(52) MASS (m/z): 641 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.81 (1H, m), 2.56(2/3×3H, s), 2.72 (1/3×3H, s), 2.97-3.07 (2H, m), 3.08 (6H, s),3.22-3.38 (1H, m), 3.38-3.78 (8H, m), 3.80 (1/3×1H, d, J=17 Hz), 4.27(1/3×1H, d, J=17 Hz), 4.32 (2/3×2H, ABq, Δ=0.24, J=15 Hz), 4.98-5.30(2H, m), 6.42 (1/3×1H, d, J=9 Hz), 6.45 (2/3×1H, d, J=9 Hz), 7.04-8.25(14H, m)

(53) MASS (m/z): 662 (M+H)⁺ ; NMR (CDCl₃, δ): 2.55-2.71 (1H, m), 2.68(3/4×3H, s), 2.82 (1/4×3H, s), 2.92-3.14 (2H, m), 3.20-3.35 (1H, m),3.35-3.76 (8H, m), 4.27 (1/4×2H, ABq, Δ=0.20, J=17 Hz), 4.49 (3/4×2H,ABq, Δ=0.20, J=15 Hz), 5.05-5.21 (2H, m), 6.95-8.13 (19H, m), 9.55 (1H,br s)

(54) MASS (m/z): 663 (M+H)⁺ ; NMR (CDCl₃, δ): 2.57-2.72 (1H, m), 2.68(3/4×3H, s), 2.81 (1/4×3H, s), 2.97-3.18 (2H, m), 3.25-3.40 (1H, m),3.40-3.82 (8H, m), 4.26 (1/4×2H, ABq, Δ=0.20, J=17 Hz), 4.49 (3/4×2H,ABq, Δ=0.17, J=15 Hz), 5.03-5.20 (2H, m), 7.00-7.88 (18H, m), 8.14-8.27(1H, m)

(55) MASS (m/z): 664 (M+H)⁺ ; NMR (CDCl₃, δ): 2.58 (2/5×3H, s),2.60-2.73 (1H, m), 2.62 (3/5×3H, s), 2.65 (3/5×3H, s), 2.80 (2/5×3H, s),2.92-3.12 (2H, m), 3.17-3.30 (1H, m), 3.36-3.74 (8H, m), 3.70 (3H, s),4.12 (2/5×1H, d, J=17 Hz), 4.43 (3/5×1H, d, J=15 Hz), 4.57 (2/5×1H, d,J=17 Hz), 4.75 (3/5×1H, d, J=15 Hz), 5.02-5.32 (2H, m), 6.88-8.13 (15H,m), 9.78 (2/5×1H, s), 10.52 (3/5×1H, s)

(56) MASS (m/z): 665 (M+H)⁺ ; NMR (CDCl₃, δ): 2.58-2.72 (1H, m), 2.58(3H, s), 2.60 (2/3×3H, s), 2.78 (1/3×3H, s), 2.92-3.14 (2H, m),3.22-3.38 (1H, m), 3.40-3.80 (8H, m), 3.70 (3H, s), 4.13 (1/3×1H, d,J=17 Hz), 4.48 (2/3×1H, d, J=15 Hz), 4.53 (1/3×1H, d, J=17 Hz), 4.69(2/3×1H, d, J=15 Hz), 5.02-5.30 (2H, m), 6.85-7.80 (14H, m), 8.15-8.28(1H, m)

(57) MASS (m/z): 586 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53-3.00 (3H, m), 2.87(2/3×3H, s), 2.89 (1/3×3H, s), 3.16-3.33 (1H, m), 3.33-3.76 (8H, m),4.32 (2/3×1H, d, J=15 Hz) 4.51 (1/3×2H, ABq, Δ=0.05, J=17 Hz), 4.72(2/3×1H, d, J=15 Hz), 5.01-5.22 (2H, m), 6.18 (1/3×1H, s), 6.22 (2/3×1H,s), 6.92-8.14 (14H, m), 9.66 (1/3×1H, br s), 9.70 (2/3×1H, br s)

(58) MASS (m/z): 587 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53-3.05 (3H, m), 2.88(3H, s), 3.22-3.80 (9H, m), 4.35 (2/3×1H, d, J=15 Hz), 4.51 (1/3×2H,ABq, Δ=0.06, J=17 Hz), 4.70 (2/3×1H, d, J=15 Hz), 4.98-5.18 (2H, m),6.21 (1/3×1H, s), 6.27 (2/3×1H, s), 7.03-7.74 (13H, m), 8.22 (1H, d, J=8Hz)

(59) MASS (m/z): 600 (M+H)⁺ ; NMR (CDCl₃, δ): 2.59-2.73 (1H, m), 2.63(2/3×3H, s), 2.81 (1/3×3H, s), 2.92-3.14 (2H, m), 3.18-3.32 (1H, m),3.37-3.75 (8H, m), 3.81 (1/3×3H, s), 3.84 (2/3×3H, s), 4.08 (1/3×2H,ABq, Δ=0.18, J=17 Hz), 4.12 (2/3×1H, d, J=15 Hz), 4.42 (2/3×1H, d, J=15Hz), 5.00-5.28 (2H, m), 6.95-8.10 (14H, m), 9.68 (1H, br s)

(60) MASS (m/z): 601 (M+H)⁺ ; NMR (CDCl₃, δ): 2.56-2.72 (1H, m), 2.62(2/3×3H, s), 2.80 (1/3×3H, s), 2.90-3.18 (2H, m), 3.24-3.38 (1H, m),3.38-3.80 (8H, m), 3.82 (1/3×3H, s), 3.85 (2/3×3H, s), 4.06 (1/3×2H,ABq, Δ=0.20, J=17 Hz), 4.13 (2/3×1H, d, J=15 Hz), 4.42 (2/3×1H, d, J=15Hz), 4.98-5.25 (2H, m), 6.98-7.72 (13H, m), 8.13-8.25 (1H, m)

(61) MASS (m/z): 630 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52-2.92 (1H, m), 2.72(2/3×3H, s), 2.85-3.08 (2H, m), 2.87 (1/3×3H, s), 3.13-3.30 (1H, m),3.33-3.75 (8H, m), 4.21 (2/3×1H, d, J=15 Hz), 4.41 (1/3×2H, ABq, Δ=0.07,J=17 Hz), 4.74 (2/3×1H, d, J=15 Hz), 5.04-5.25 (2H, m), 6.90-8.12 (16H,m), 9.77 (1/3×1H, s), 9.82 (2/3×1H, s)

(62) MASS (m/z): 631 (M+H)⁺ ; NMR (CDCl₃, δ): 2.51-2.78 (1H, m), 2.72(2/3×3H, s), 2.84 (1/3×3H, s), 2.85-3.11 (2H, m), 3.20-3.37 (1H, m),3.37-3.82 (8H, m), 4.25 (2/3×1H, d, J=15 Hz), 4.40 (1/3×2H, s), 4.71(2/3×1H, d, J=15 Hz), 4.98-5.18 (2H, m), 6.90-7.74 (15H, m), 8.20 (1H,d, J=9 Hz)

(63) MASS (m/z): 586 (M+H)⁺ ; NMR (CDCl₃, δ): 2.53-2.75 (1H, m), 2.80(2/3×3H, s), 2.87 (1/3×3H, s), 2.95-3.31 (3H, m), 3.31-3.78 (8H, m),4.24 (2/3×1H, d, J=15 Hz), 4.45 (1/3×2H, ABq, Δ=0.13, J=17 Hz), 4.81(2/3×1H, d, J=15 Hz), 5.08-5.32 (2H, m), 5.97-6.21 (2H, m), 6.92-8.15(13H, m), 9.82 (1/3×1H, br s), 9.88 (2/3×1H, br s)

(64) MASS (m/z): 587 (M+H)⁺ ; NMR (CDCl₃, δ): 2.52-2.72 (1H, m), 2.79(2/3×3H, s), 2.85 (1/3×3H, s), 2.96-3.19 (2H, m), 3.21-3.38 (1H, m),3.38-3.82 (8H, m), 4.29 (2/3×1H, d, J=15 Hz), 4.43 (1/3×2H, ABq, Δ=0.17,J=17 Hz), 4.77 (2/3×1H, d, J=15 Hz), 5.01-5.28 (2H, m), 6.03-6.27 (2H,m), 7.07-7.80 (12H, m), 8.15-8.30 (1H, m)

(65) MASS (m/z): 603 (M+H)⁺ ; NMR (CDCl₃, δ): 2.51-2.70 (1H, m), 2.81(2/3×3H, s), 2.86 (1/3×3H, s), 2.96-3.18 (2H, m), 3.18-3.38 (1H, m),3.38-3.82 (8H, m), 4.30 (2/3×1H, d, J=15 Hz), 4.45 (1/3×2H, ABq, Δ=0.18,J=17 Hz), 4.77 (2/3×1H, d, J=15 Hz), 4.96-5.25 (2H, m), 6.05-6.25 (2H,m), 7.05-8.22 (13H, m)

(66) MASS: 648 (M+1); NMR (CDCl₃, δ): 2.60-2.78 (1H, m), 2.70 (3×2/3H,s), 2.85 (3×1/3H, s), 2.95-3.12 (2H, m), 3.13-3.30 (1H, m), 3.31-3.50(2H, m), 3.51-3.90 (6H, m), 4.36 (2×1/6H, d, J=16 Hz), 4.55 (2×1/6H, d,J=16 Hz), 4.61 (2×1/3H, d, J=15 Hz), 4.73 (2×1/3H, d, J=15 Hz),5.10-5.33 (2H, m), 6.95-7.35 (8H, m), 7.36-7.50 (2H, m), 7.62 (1H, d,J=8 Hz), 7.78 (1×1/3H, s), 7.83 (1×2/3H, s), 7.93-8.20 (3H, m), 8.81(2H, s)

(67) MASS: 649 (M+1); NMR (CDCl₃, δ): 2.61-2.70 (1H, m), 2.71 (3×2/3H,s), 2.88 (3×1/3H, s), 3.00-3.18 (2H, m), 3.29 (1H, t, J=15 Hz),3.40-3.59 (2H, m), 3.60-3.80 (6H, m), 4.38 (2×1/6H, d, J=16 Hz), 4.58(2×1/6H, d, J=16 Hz), 4.62 (2×1/3H, d, J=15 Hz), 4.79 (2×1/3H, d, J=15Hz), 5.08-5.22 (2H, m), 7.11-7.25 (5H, m), 7.26-7.37 (1H, m), 7.40-7.50(2H, m), 7.51 (1H, s), 7.56 (1H, d, J=8 Hz), 7.68 (1H, d, J=8 Hz),7.75-7.90 (2H, m), 8.02 (1H, d, J=8 Hz), 8.20 (1×1/3H, d, J=8 Hz), 8.23(1×2/3H, d, J=8 Hz), 8.80 (2H, s)

(68) MASS: 646 (M+1); NMR (CDCl₃, δ): 2.02 (3×2/3H, s), 2.68 (3×1/3H,s), 2.71-2.90 (1H, m), 3.17-3.50 (5H, m), 3.51-3.70 (6H, m), 3.67(2×1/6H, d, J=16 Hz), 3.96 (2×1/6H, d, J=16 Hz), 4.18 (2×1/3H, d, J=15Hz), 4.50 (2×1/3H, d, J=15 Hz), 5.27-5.50 (2H, m), 6.71-6.80 (2×1/3H,m), 6.90-7.00 (2×2/3H, m), 7.01-7.32 (8H, m), 7.33-7.57 (3H, m),7.60-7.70 (2H, m), 7.74 (1H, d, J=8 Hz), 7.93-8.12 (1H, m), 8.24(2×1/3H, d, J=8 Hz), 8.31 (2×2/3H, d, J=8 Hz)

(69) MASS: 647 (M+1); NMR (CDCl₃, δ): 1.99 (3×2/3H, s), 2.61 (3×1/3H,s), 2.58-2.74 (1H, m), 3.28-3.60 (5H, m), 3.60-3.80 (6H, m), 3.72(2×1/6H, d, J=16 Hz), 3.89 (2×1/6H, d, J=16 Hz), 4.19 (2×1/3H, d, J=15Hz), 4.40 (2×1/3H, d, J=15 Hz), 5.08-5.22 (1H, m), 5.27-5.40 (1H, m),6.68-6.78 (2×1/3H, m), 6.90-6.99 (2×2/3H, m), 7.10-7.37 (6H, m),7.38-7.62 (5H, m), 7.62-7.90 (4H, m), 8.10-8.40 (2H, m)

(70) MASS: 598 (M+1); NMR (CDCl₃, δ): 2.53-2.70 (1H, m), 2.71 (3×2/3H,s), 2.85 (3×1/3H, s), 2.90-3.15 (2H, m), 3.22-3.35 (1H, m), 3.37-3.58(2H, m), 3.60-3.80 (6H, m), 4.37 (2×1/3H, d, J=15 Hz), 4.38 (2×1/6H, d,J=16 Hz), 4.43 (2×1/6H, d, J=16 Hz), 4.60 (2×1/3H, d, J=15 Hz),5.00-5.20 (2H, m), 7.98-8.18 (3H, m), 7.22-7.38 (4H, m), 7.40-7.73 (6H,m), 8.20 (1H, d, J=8 Hz), 8.33 (1×1/3H, s), 8.44 (1H, d, J=2 Hz), 8.49(1×2/3H, s)

(71) MASS: 597 (M+1); NMR (CDCl₃, δ): 2.58-2.75 (1H, m), 2.78 (3×2/3H,s), 2.88 (3×1/3H, s), 2.91-3.30 (3H, m), 3.31-3.50 (2H, m), 3.51-3.70(6H, m), 4.31 (2×1/3H, d, J=15 Hz), 4.42 (2×1/6H, d, J=16 Hz), 4.51(2×1/6H, d, J=16 Hz), 4.67 (2×1/3H, d, J=15 Hz), 5.10-5.30 (2H, m),6.90-7.18 (5H, m), 7.20-7.33 (4H, m), 7.34-7.50 (2H, m), 7.64 (1H, d,J=8 Hz), 7.95-8.10 (2H, m), 8.32 (1×1/3H, s), 8.43 (1×2/3H, s), 8.45(1H, s)

(72) MASS: 658 (M+1); NMR (CDCl₃, δ): 2.27 (3H, s), 2.31-2.48 (4H, m),2.52 (3×2/3H, s), 2.64-2.80 (1H, m), 2.70 (3×1/3H, s), 2.93-3.15 (2H,m), 3.29 (1H, d, J=15 Hz), 3.39-3.57 (2H, m), 3.58-3.73 (2H, m), 3.88(3H, s), 4.18 (2×1/6H, d, J=16 Hz), 4.19 (2×1/3H, d, J=15 Hz), 4.23(2×1/6H, d, J=16 Hz), 4.49 (2×1/3H, d, J=15 Hz), 4.98-5.22 (2H, m), 6.61(1×1/3H, d, J=8 Hz), 6.63 (1×2/3H, d, J=8 Hz), 7.00-7.37 (6H, m),7.40-7.60 (2H, m), 7.68 (1×1/3H, d, J=8 Hz), 7.70 (1×2/3H, d, J=8 Hz),7.81 (1×1/3H, s), 7.90 (1×2/3H, s), 7.93 (1H, d, J=8 Hz), 8.11 (1H, d,J=8 Hz), 8.80 (1H, d, J=8 Hz)

(73) MASS: 563 (M+1); NMR (CDCl₃, δ): 0.70-0.95 (3H, m), 1.15-1.45 (4H,m), 1.55-1.85 (2H, m), 2.60-2.72 (1H, m), 2.90 (3×1/3H, s), 3.00(3×2/3H, s), 3.30 (1H, d, J=15 Hz), 3.38-3.58 (2H, m), 3.58-3.77 (6H,m), 4.38 (2×1/3H, d, J=15 Hz), 4.62 (2×1/3H, s), 4.76 (2×1/3H, d, J=15Hz), 4.83-4.99 (1H, m), 5.05-5.20 (1H, m), 7.10-7.37 (5H, m), 7.37-7.46(2H, m), 7.49-7.60 (2H, m), 7.61-7.78 (2H, m), 8.27 (1H, d, J=8 Hz)

(74) MASS: 562 (M+1); NMR (CDCl₃, δ): 0.60-0.90 (3H, m), 1.03-1.38 (4H,m), 1.50-1.80 (2H, m), 2.60-2.75 (1H, m), 2.88 (3×1/3H, s), 2.91(3×2/3H, s), 3.10-3.28 (1H, m), 3.29-3.43 (2H, m), 3.44-3.68 (6H, m),4.22 (2×1/3H, d, J=15 Hz), 4.52 (2×1/6H, d, J=16 Hz), 4.61 (2×1/6H, d,J=16 Hz), 4.80 (2×1/3H, d, J=15 Hz), 4.86-5.00 (1H, m), 5.12-5.35 (1H,m), 7.01 (1H, s), 7.03-7.38 (7H, m), 7.42 (1H, d, J=8 Hz), 7.62 (1H, d,J=8 Hz), 7.97 (1×1/3H, d, J=8 Hz) 8.07 (1×2/3H, d, J=8 Hz), 8.11 (1H, d,J=8 Hz)

(75) MASS: 644 (M+1); NMR (CDCl₃, δ): 2.58-2.70 (1H, m), 2.61 (3×2/3H,s), 2.73 (3×1/3H, s), 2.97-3.12 (2H, m), 3.22-3.34 (1H, m), 3.40-3.58(2H, m), 3.60-3.78 (6H, m), 3.87 (3H, s), 4.22 (2×1/3H, d, J=15 Hz),4.23 (2×1/6H, d, J=16 Hz), 4.31 (2×1/6H, d, J=16 Hz), 4.51 (2×1/3H, d,J=15 Hz), 5.02-5.21 (2H, m), 6.61-6.70 (1H, m), 7.08-7.23 (5H, m),7.30-7.50 (3H, m), 7.72-7.98 (5H, m), 8.13 (1H, d, J=8 Hz)

EXAMPLE 38

The following compound was obtained according to a similar manner tothat of Example 8.

MASS (m/z): 610 (M+H)⁺ ; NMR (CDCl₃, δ): 2.2-2.3 (2H, m), 2.4-2.6 (2H,m), 2.73 (2/3×3H, s), 2.93 (1/3×3H, s), 3.0-3.1 (2H, m), 3.3-3.6 (8H,m), 4.2-4.8 (2H, m), 5.0-5.1 (1H, m), 5.2-5.3 (1H, m), 7.0-7.7 (15H, m),7.72 (1H, br s), 8.05 (1H, br s), 8.50 (1H, br s) (1H, m), 5.2-5.3 (1H,m), 7.0-7.7 (15H, m), 7.72 (1H, br s), 8.05 (1H, br s), 8.50 (1H, br s)

EXAMPLE 39

To a mixture of Starting Compound (112 mg) and triethylamine (70 μl) indichloromethane (1.2 ml) was added (benzofuran-2-yl)sulfonyl chloride(68 mg) with ice-cooling. The mixture was stirred at room temperaturefor 12 hours then subjected to column chromatography (silica gel,chloroform/methanol=50/1) to give Object Compound (130 mg) as a whitepowder.

MASS (m/z): 633 (M+H)⁺ ; NMR (CDCl₃, δ): 2.38-2.59 (1H, m), 2.52(2/3×3H, s), 2.73 (1/3×3H, s), 2.81-3.04 (2H, m), 3.04-3.72 (9H, m),3.98 (1/3×1H, d, J=17 Hz), 4.24 (1/3×1H, d, J=17 Hz), 4.25 (2/3×1H, d,J=15 Hz), 4.28-4.44 (1H, m), 4.57 (2/3×1H, d, J=15 Hz), 4.88-5.05 (1H,m), 6.78-6.90 (17H, m)

EXAMPLE 40

The following object compounds were obtained according to a similarmanner to that of Example 39.

(1) MASS (m/z): 571 (M+H)⁺ ; NMR (CDCl₃, δ): 2.61 (3/4×3H, s), 2.74(1/4×3H, s), 2.78-3.05 (2H, m), 3.50-3.78 (2H, m), 3.87-4.04 (1H, m),3.88 (1/4×1H, d, J=17 Hz), 4.12 (1H, br s), 4.30 (1/4×1H, d, J=17 Hz),4.42 (3/4×2H, ABq, Δ=0.14, J=15 Hz), 4.90-5.05 (1H, m), 6.45 (1H, br s),6.96-7.72 (13H, m), 8.00-8.22 (1H, m)

(2) MASS (m/z): 598 (M+H)⁺ ; NMR (CDCl₃, δ): 2.51 (3/4×3H, s), 2.58-2.95(2H, m), 2.72 (1/4×3H, s), 2.95-3.34 (2H, m), 4.08 (1/4×2H, ABq, Δ=0.21,J=17 Hz), 4.24 (3/4×1H, d, J=15 Hz), 4.31-4.44 (1H, m), 4.55 (3/4×1H, d,J=15 Hz), 4.90-5.06 (1H, m), 6.90-7.85 (17H, m), 8.14-8.55 (3H, m)

(3) MASS (m/z): 646 (M+H)⁺ ; NMR (CDCl₃, δ): 2.11-2.40 (4H, m), 2.25(3H, s), 2.40-2.58 (1H, m), 2.50 (2/3×3H, s), 2.73 (1/3×3H, s),2.82-3.05 (2H, m), 3.13-3.70 (5H, m), 4.11 (1/3×2H, ABq, Δ=0.25, J=17Hz), 4.22 (2/3×1H, d, J=15 Hz), 4.25-4.41 (1H, m), 4.58 (2/3×1H, d, J=15Hz), 4.89-5.05 (1H, m), 6.78-7.90 (17H, m)

EXAMPLE 41

The following object compounds were obtained according to a similarmanner to that of Example 1.

(1) MASS: 573 (M+1); NMR (CDCl₃, δ): 2.00 (3×1/3H, s), 2.01 (3×2/3H, s),2.70 (3×2/3H, s), 2.91 (3×1/3H, s), 2.93-3.07 (2H, m), 3.07-3.23 (2H,m), 4.22 (2×1/3H, s), 4.27 (2×1/3H, d, J=15 Hz), 4.97 (2×1/3H, d, J=15Hz), 5.10-5.40 (1H, m), 5.60-5.80 (1H, m), 6.78 (1H, d, J=8 Hz), 6.82(1H, d, J=8 Hz), 6.89-7.18 (11H, m), 7.18-7.40 (5H, m), 7.48 (1H, d, J=8Hz), 7.67 (1H, d, J=8 Hz), 8.99 (1H, t, J=8 Hz)

(2) MASS: 574 (M+1); NMR (CDCl₃, δ): 2.22 (3H, s), 2.60 (3×2/3H, s),2.83 (3×1/3H, s), 2.90-3.03 (2H, m), 3.08-3.20 (2H, m), 4.11 (2×1/6H, d,J=16 Hz), 4.27 (2×1/6H, d, J=16 Hz), 4.32 (2×1/3H, d, J=15 Hz), 4.62(2×1/3H, d, J=15 Hz), 4.95-5.08 (1H, m), 5.10-5.21 (1H, m), 6.90-7.33(17H, m), 7.40 (1H, t, J=8 Hz), 7.43-7.56 (2H, m), 7.68 (1H, d, J=8 Hz)

(3) MASS: 571 (M+1); NMR (CDCl₃, δ): 2.78 (3×1/4H, s), 3.00 (3×3/4H, s),2.90-3.30 (2H, m), 3.30-3.48 (1H, m), 4.40-4.53 (1H, m), 4.54-4.77 (2H,m), 4.78-4.98 (2H, m), 5.10-5.20 (1H, m), 5.50-5.68 (1H, m), 6.70-7.50(19H, m), 7.58 (1×3/4H, d, J=8 Hz), 7.72 (1×1/4H, d, J=8 Hz), 9.73(1×1/4H, s), 9.82 (1×3/4H, s)

(4) MASS: 517 (M+1); NMR (CDCl₃, δ): 0.75 (3×1/5H, t, J=8 Hz), 0.81(3×4/5H, t, J=8 Hz), 1.08-1.48 (4H, m), 1.62-1.90 (2H, m), 2.99 (3×1/5H,s), 3.11 (3×4/5H, s), 3.70-3.90 (1H, m), 4.01-4.22 (1H, m), 4.73(2×1/2H, d, J=15 Hz), 4.82 (2×1/2H, d, J=15 Hz), 4.83-5.10 (3H, m), 7.27(1H, t, J=7 Hz), 7.38 (1H, t, J=8 Hz), 7.42-7.53 (3H, m), 7.54-7.90 (5H,m), 7.98-8.18 (2H, m), 8.80 (1×4/5H, d, J=2 Hz), 8.90 (1×1/5H, d, J=2Hz)

(5) MASS: 516 (M+1); NMR (CDCl₃, δ): 0.69 (3×1/5H, t, J=8 Hz), 0.79(3×4/5H, t, J=8 Hz), 1.08-1.45 (4H, m), 1.60-2.01 (2H, m), 3.10 (3×1/5H,s), 3.22 (3×4/5H, s), 3.90-4.16 (2H, m), 4.60 (2×2/5H, d, J=15 Hz), 4.71(2×1/5H, s), 5.01 (2×2/5H, d, J=15 Hz), 4.82-5.15 (1H, m), 5.50-5.70(1H, m), 6.58 (1×1/5H, s), 6.71 (1×4/5H, s), 6.92-7.20 (3H, m),7.30-7.42 (3H, m), 7.50 (1H, d, J=8 Hz), 7.51-7.78 (2H, m), 71.81 (1H,s), 7.93 (1H, d, J=8 Hz), 8.71 (1×4/5H, s), 8.82 (1×1/5H, s), 8.90(1×1/5H, d, J=8 Hz), 9.00 (1×4/5H, d, J=8 Hz)

(6) MASS: 578 (M+1); NMR (CDCl₃, δ): 0.72 (3×1/4H, t, J=8 Hz), 0.78(3×3/4H, t, J=8 Hz), 1.16-1.36 (4H, m), 1.49-1.80 (2H, m), 2.92 (3×1/4H,s), 3.00 (3×3/4H, s), 3.28-3.52 (2H, m), 4.58 (2×3/8H, d, J=15 Hz), 4.79(2×1/8H, d, J=16 Hz), 4.85 (2×1/8H, d, J=16 Hz), 4.90 (2×3/8H, d, J=15Hz), 4.83-5.01 (1H, m), 5.02-5.18 (1H, m), 7.18 (1H, t, J=8 Hz),7.21-7.35 (2H, m), 7.41 (1H, t, J=8 Hz), 7.48-7.89 (7H, m), 7.95-8.23(3H, m), 8.59 (1H, d, J=4 Hz), 8.73 (1H, d, J=2 Hz), 8.79 (1H, d, J=8Hz)

(7) MASS: 577 (M+1); NMR (CDCl₃, δ): 0.62 (3×1/4H, t, J=8 Hz), 0.68(3×3/4H, t, J=8 Hz), 0.95-1.30 (4H, m), 1.38-1.57 (1H, m), 1.58-1.72(1H, m), 2.92 (3×1/4H, s), 2.98 (3×3/4H, s), 2.98-3.50 (2H, m), 4.63(2×3/8H, d, J=15 Hz), 4.64 (2×1/8H, d, J=16 Hz), 4.78 (2×3/8H, d, J=15Hz), 4.81 (2×1/8H, d, J=16 Hz), 4.82-5.05 (1H, m), 5.17-5.38 (1H, m),6.97-7.12 (3H, m), 7.13-7.22 (2H, m), 7.32-7.59 (3H, m), 7.60-7.80 (3H,m), 7.94 (1H, s), 8.06-8.18 (2H, m), 8.41 (1×1/4H, d, J=8 Hz), 8.48(1×1/4H, d, J=4 Hz), 8.51 (1×3/4H, d, J=4 Hz), 8.69 (1×3/4H, d, J=8 Hz),8.73 (1×3/4H, d, J=2 Hz), 8.78 (1×1/4H, d, J=2 Hz)

(8) MASS: 575 (M+1); NMR (CDCl₃, δ): 2.06-2.28 (2H, m), 2.1O (3H, s),2.50-2.70 (2H, m), 2.61 (3×2/3H, s), 2.81 (3×1/3H, s), 2.92-3.12 (2H,m), 3.91 (3H, s), 3.99 (2×1/6H, d, J=16 Hz), 4.31 (2×1/3H, d, J=15 Hz),4.32 (2×1/6H, d, J=16 Hz), 4.52 (2×1/3H, d, J=15 Hz), 4.97 (1H, q, J=8Hz), 5.12 (1×2/3H, q, J=8 Hz), 5.27 (1×1/3H, q, J=8 Hz), 6.67 (1×1/3H,d, J=8 Hz), 6.69 (1×2/3H, d, J=8 Hz), 7.05-7.21 (5H, m), 7.22-7.48 (5H,m), 7.51 (1H, d, J=8 Hz), 7.54 (1H, s), 7.69 (1H, d, J=8 Hz), 7.89(1×1/3H, d, J=2 Hz), 7.99 (1×2/3H, d, J=2 Hz)

(9) MASS: 591 (M+1); NMR (CDCl₃, δ): 2.07-2.23 (2H, m), 2.09 (3H, s),2.50-2.72 (2H, m), 2.65 (3×2/3H, s), 2.79 (3×1/3H, s), 2.92-3.12 (2H,m), 3.89 (3H, s), 3.94 (2×1/6H, d, J=16 Hz), 4.29 (2×1/3H, d, J=15 Hz),4.33 (2×1/6H, d, J=16 Hz), 4.51 (2×1/3H, d, J=15 Hz), 4.91 (1H, q, J=8Hz), 5.11 (1×2/3H, q, J=8 Hz), 5.25 (1×1/3H, q, J=8 Hz), 6.63 (1×1/3H,d, J=8 Hz), 6.67 (1×2/3H, d, J=8 Hz), 7.02-7.21 (5H, m), 7.30-7.60 (5H,m), 7.73-7.90 (3H, m), 7.87 (1×1/3H, d, J=2 Hz), 7.98 (1×2/3H, d, J=2Hz)

(10) MASS: 574 (M+1); NMR (CDCl₃, δ): 2.07 (3×2/3H, s), 2.08 (3×1/3H,s), 2.10-2.41 (2H, m), 2.53-2.68 (2H, m), 2.70 (3×2/3H, s), 2.93-3.12(2H, m), 2.97 (3×1/3H, s), 3.91 (3×1/3H, s), 3.92 (3×2/3H, s), 4.02(2×1/6H, d, J=16 Hz), 4.32 (2×1/6H, d, J=16 Hz), 4.42 (2×1/3H, d, J=15Hz), 4.70 (2×1/3H, d, J=15 Hz), 5.30-5.50 (1H, m), 5.51-5.62 (1H, m),6.63 (1×1/3H, d, J=8 Hz), 6.69 (1×2/3H, d, J=8 Hz), 6.93-7.18 (7H, m),7.19-7.40 (3H, m), 7.50 (1H, d, J=8 Hz), 7.69 (1H, d, J=8 Hz), 7.89(1×1/3H, d, J=2 Hz), 8.02 (1×2/3H, d, J=2 Hz), 9.03 (1×2/3H, d, J=8 Hz),9.11 (1×1/3H, d, J=8 Hz)

(11) MASS: 561 (M+1); NMR (CDCl₃, δ): 0.72 (3×1/4H, t, J=8 Hz), 0.80(3×3/4H, t, J=8 Hz), 1.10-1.40 (4H, m), 1.60-1.90 (2H, m), 2.08 (3H, s),2.12-2.28 (2H, m), 2.53-2.73 (2H, m), 3.01 (3×1/4H, s), 3.11 (3×3/4H,s), 4.70 (2×3/8H, d, J=15 Hz), 4.89 (2×1/4H, s), 4.91 (2×3/8H, d, J=15Hz), 4.93-5.11 (2H, m), 7.20-7.33 (1H, m), 7.34-7.60 (6H, m), 7.60-7.89(3H, m), 8.01 (1H, s), 8.10 (1×3/4H, d, J=8 Hz), 8.12 (1×1/4H, d, J=8Hz), 8.81 (1×3/4H, s), 8.88 (1×1/4H, s)

(12) MASS: 560 (M+1); NMR (CDCl₃, δ): 0.59 (3×1/4H, t, J=8 Hz), 0.65(3×3/4H, t, J=8 Hz), 0.98-1.50 (4H, m), 1.58-1.90 (2H, m), 2.00 (3×3/4H,s), 2.02 (3×1/4H, s), 2.10-2.33 (2H, m), 2.52-2.80 (2H, m), 3.13 (3H,s), 4.79 (2×3/8H, d, J=15 Hz), 4.91 (2×1/4H, s), 5.10 (2×3/8H, d, J=15Hz), 5.12-5.31 (1H, m), 5.43-5.60 (1H, m), 6.96-7.18 (3H, m), 7.27-7.47(2H, m), 7.50-7.68 (2H, m), 7.69-7.90 (2H, m), 8.00 (1×1/4H, s), 8.06(1×3/4H, s), 8.11 (1H, d, J=8 Hz), 8.72-9.00 (2H, m)

(13) MASS: 566 (M+1); NMR (CDCl₃, δ): 0.58 (3×1/4H, t, J=8 Hz), 0.63(3×3/4H, t, J=8 Hz), 0.93-1.37 (4H, m), 1.50-1.80 (2H, m), 3.00 (3×1/4H,s), 3.07 (3×3/4H, s), 3.12-3.28 (2H, m), 4.61 (2×3/8H, d, J=15 Hz), 4.71(2×1/8H, d, J=16 Hz), 4.87 (2×3/8H, d, J=15 Hz), 4.99 (2×1/8H, d, J=16Hz), 4.90-5.10 (1H, m), 5.30-5.50 (1H, m), 6.69 (1×3/4H, s), 6.73(1×1/4H, s), 6.94-7.20 (3H, m), 7.32 (1×3/4H, s), 7.36 (1×1/4H, s), 7.40(1H, s), 7.48-7.61 (2H, m), 7.62-7.90 (3H, m), 7.99 (1H, s), 8.09 (1H,d, J=8 Hz), 8.53-8.70 (1H, m), 8.75 (1H, s)

(14) MASS: 567 (M+1); NMR (CDCl₃, δ): 0.70 (3×1/4H, t, J=8 Hz), 0.78(3×3/4H, t, J=8 Hz), 1.00-1.40 (4H, m), 1.57-1.85 (2H, m), 3.01 (3×1/4H,s), 3.11 (3×3/4H, s), 3.03-3.33 (2H, m), 4.65-4.97 (3H, m), 4.98-5.10(1H, m), 6.81 (1H, s), 7.18-7.30 (2H, m), 7.40 (1H, t, J=8 Hz),7.42-7.90 (6H, m), 8.01 (1H, s), 8.10 (2H, d, J=8 Hz), 8.2-8.40 (1H, m),8.80 (1×3/4H, s), 8.87 (1×1/4H, s)

(15) MASS: 530 (M+1); NMR (CDCl₃, δ): 2.70 (3×4/5H, s), 2.88 (3×1/5H,s), 3.00-3.20 (2H, m), 3.88 (3H, s), 3.91-4.08 (2H, m), 4.16 (2×1/10H,d, J=16 Hz), 4.30 (2×1/10H, d, J=16 Hz), 4.47 (2×4/5H, s), 4.81 (1H, brs), 5.30 (1×4/5H, q, J=8 Hz), 5.39 (1×1/5H, q, J=8 Hz), 5.59 (1H, q, J=8Hz), 6.49 (1×4/5H, d, J=8 Hz), 6.61 (1×1/5H, d, J=8 Hz), 6.97-7.41 (10H,m), 7.48 (1H, d, J=8 Hz), 7.68 (1×1/5H, d, J=8 Hz), 7.86 (1×4/5H, d, J=2Hz), 7.90 (1H, d, J=2 Hz), 9.01 (1×1/5H, d, J=8 Hz), 9.05 (1×4/5H, d,J=8 Hz)

(16) MASS: 531 (M+1); NMR (CDCl₃, δ): 2.68 (3×3/4H, s), 2.81 (3×1/4H,s), 2.92-3.17 (2H, m), 3.69-3.80 (1H, m), 3.90 (3H, s), 4.00 (2×1/8H, d,J=16 Hz), 4.03-4.18 (1H, m), 4.30 (2×3/8H, d, J=15 Hz), 4.41 (2×1/8H, d,J=16 Hz), 4.52 (2×3/8H, d, J=15 Hz), 4.73-4.88 (1H, m), 5.12 (1×3/4H, q,J=8 Hz), 5.23 (1×1/4H, q, J=8 Hz), 6.69 (1×3/4H, d, J=8 Hz), 6.70(1×1/4H, d, J=8 Hz), 7.00-7.21 (6H, m), 7.28 (1H, t, J=8 Hz), 7.32-7.48(2H, m), 7.48-7.72 (4H, m), 7.92 (1×1/4H, d, J=2 Hz), 7.98 (1×3/4H, d,J=2 Hz)

(17) MASS: 531 (M+1); NMR (CDCl₃, δ): 2.49 (3H, s), 2.62 (3×3/4H, s),2.74 (3×1/4H, s), 2.92-3-15 (2H, m), 3.73-3.88 (1H, m), 3.97 (2×1/8H, d,J=16 Hz), 4.01-4.18 (1H, m), 4.36 (2×3/8H, d, J=15 Hz), 4.48 (2×1/8H, d,J=16 Hz), 4.49 (2×3/8H, d, J=15 Hz), 4.70-4.97 (2H, m), 5.11 (1×3/4H, q,J=8 Hz), 5.21 (1×1/4H, q, J=8 Hz), 6.98-7.20 (6H, m), 7.20-7.42 (3H, m),7.49 (1×3/4H, s), 7.51 (1×1/4H, s), 7.70-7.87 (3H, m), 7.91 (1×3/4H, d,J=8 Hz), 7.95 (1×1/4H, d, J=8 Hz), 8.27 (1H, s)

(18) MASS: 671 (M+1); NMR (CDCl₃, δ): 1.38 (3H, t, J=8 Hz), 2.30 (3H,s), 2.32-2.51 (4H, m), 2.52-2.70 (1H, m), 2.53 (3×3/4H, s), 2.73(3×1/4H, s), 2.93-3.13 (2H, m), 3.32 (1H, dd, J=17, 2 Hz), 3.40-3.59(2H, m), 3.60-3.75 (2H, m), 3.93 (2×1/8H, d, J=16 Hz), 4.18 (2×3/8H, d,J=15 Hz), 4.26 (2×1/8H, d, J=16 Hz), 4.31 (2H, q, J=8 Hz), 4.51 (2×3/8H,d, J=15 Hz), 4,98-5.20 (2H, m), 6.60 (1×1/4H, d, J=8 Hz), 6.62 (1×3/4H,d, J=8 Hz), 7.00-7.22 (5H, m), 7.29 (1H, dd, J=12, 2 Hz), 7.32-7.48 (2H,m), 7.68-7.96 (5H, m), 8.14 (1H, d, J=8 Hz)

(19) MASS: 610 (M+1); NMR (CDCl₃, δ): 2.10 (3H, s), 2.55-2.80 (1H, m),2.68 (3×3/4H, s), 2.82 (3×1/4H, s), 2.88-3.08 (2H, m), 3.09-3.21 (1H,m), 3.22-3.41 (2H, m), 3.42-3.70 (6H, m), 4.23 (2×3/8H, d, J=15 Hz),4.30 (2×1/8H, d, J=16 Hz), 4.39 (2×1/8H, d, J=16 Hz), 4.73 (2×3/8H, d,J=15 Hz), 5.10-5.22 (1H, m), 5.23-5.40 (1H, m), 6.73-7.13 (9H, m),7.14-7.30 (3H, m), 7.41 (1H, d, J=8 Hz), 7.61 (1H, d, J=8 Hz), 8.00(1×1/3H, d, J=8 Hz), 8.07 (1×2/3H, d, J=8 Hz), 8.20 (1×1/3H, d, J=8 Hz),8.27 (1×2/3H, d, J=8 Hz)

(20) MASS: 611 (M+1); NMR (CDCl₃, δ): 2.22 (3H, s), 2.53-2.73 (1H, m),2.62 (3×3/4H, s), 2.80 (3×1/4H, s), 2.90-3.10 (2H, m), 3.20-3.37 (1H,m), 3.38-3.58 (2H, m), 3.58-3.80 (6H, m), 4.22 (2×1/8H, d, J=16 Hz),4.30 (2×3/8H, d, J=15 Hz), 4.39 (2×1/8H, d, J=16 Hz), 4.63 (2×3/8H, d,J=15 Hz), 5.02-5.20 (2H, m), 6.87-7.13 (6H, m), 7.18-7.35 (4H, m), 7.42(1H, t, J=8 Hz), 7.51 (1H, s), 7.57 (1H, d, J=8 Hz), 7.60-7.72 (2H, m),8.21 (1H, d, J=8 Hz)

(21) MASS: 549 (M+1); NMR (CDCl₃, δ): 0.83 (3×1/3H, t, J=8 Hz), 0.92(3×2/3H, t, J=8 Hz), 1.20-1.51 (2H, m), 1.57-1.81 (2H, m), 2.58-2.72(1H, m), 2.88 (3×1/3H, s), 2.94 (3×2/3H, s), 3.30 (1H, d, J=16 Hz),3.38-3.57 (2H, m), 3.58-3.80 (6H, m), 4.39 (2×1/3H, d, J=15 Hz), 4.60(2×1/3H, s), 4.73 (2×1/3H, d, J=15 Hz), 4.82-5.01 (1H, m), 5.06-5.20(1H, m), 7.10-7.47 (7H, m), 7.48-7.60 (2H, m), 7.68 (2×2/3H, d, J=8 Hz),7.71 (2×1/3H, d, J=8 Hz), 8.27 (1H, d, J=8 Hz)

(22) MASS: 548 (M+1); NMR (CDCl₃, δ): 0.73 (3×1/3H, t, J=8 Hz), 0.81(3×2/3H, t, J=8 Hz), 1.20-1.50 (2H, m), 1.50-1.78 (2H, m), 2.60-2.73(1H, m), 2.85 (3×1/3H, s), 2.89 (3×2/3H, s), 3.19 (1H, d, J=15 Hz),3.26-3.40 (2H, m), 3.41-3.68 (6H, m), 4.21 (2×1/3H, d, J=15 Hz), 4.52(2×1/6H, d, J=16 Hz), 4.61 (2×1/6H, d, J=16 Hz), 4.80 (2×1/3H, d, J=15Hz), 4.90-5.02 (1H, m), 5.20-5.33 (1H, m), 6.84 (1×1/3H, s), 7.01(1×2/3H, s), 7.03-7.39 (7H, m), 7.43 (1H, d, J=8 Hz), 7.62 (1H, d, J=8Hz), 7.98-8.20 (2H, m)

(23) MASS: 673 (M+1); NMR (CDl₃, δ): 2.27 (3H, s), 2.32-2.47 (4H, m),2.52 (3H, s), 2.58 (3×3/4H, s), 2.58-2.70 (1H, m), 2.73 (3×1/4H, s),2.92-3.13 (2H, m), 3.23-3.40 (1H, m), 3.40-3.60 (2H, m), 3.60-3.80 (2H,m), 4.01 (2×1/8H, d, J=16 Hz), 4.21 (2×3/8H, d, J=15 Hz), 4.30 (2×1/8H,d, J=16 Hz), 4.51 (2×3/8H, d, J=15 Hz), 4.98-5.18 (2H, m), 6.98-7.23(7H, m), 7.32-7.50 (2H, m), 7.76 (1H, d, J=8 Hz), 7.79-7.93 (3H, m),8.09-8.19 (1H, m), 8.21 (1H, s)

(24) MASS: 614 (M+1); NMR (CDCl₃, δ): 0.80 (3×1/5H, t, J=8 Hz), 0.88(3×4/5H, t, J=8 Hz), 1.15-1.43 (4H, m), 1.60-1.88 (2H, m), 2.68 (1H, dd,J=17, 7 Hz), 2.98 (3×1/5H, s), 3.09 (3×4/5H, s), 3.29 (1H, dd, J=17, 2Hz), 3.38-3.56 (2H, m), 3.57-3.80 (6H, m), 4.61 (2×1/2H, d, J=15 Hz),4.89 (2×1/2H, d, J=15 Hz), 4.78-5.03 (1H, m), 5.04-5.20 (1H, m),7.21-7.33 (1H, m), 7.41 (1H, t, J=8 Hz), 7.48-7.60 (3H, m), 7.61-7.73(2H, m), 7.74-7.89 (2H, m), 8.01 (1H, s), 8.02-8.16 (1H, m), 8.28 (1H,d, J=8 Hz), 8.78 (1×4/5H, s), 8.84 (1×1/5H, s)

(25) MASS: 613 (M+1); NMR (CDCl₃, δ): 0.71 (3×1/5H, t, J=8 Hz), 0.78(3×4/5H, t, J=8 Hz), 1.03-1.40 (4H, m), 1.53-1.82 (2H, m), 2.68 (1H, dd,J=17, 7 Hz), 2.90 (3×1/5H, s), 2.93 (3×4/5H, s), 3.23 (1H, d, J=15 Hz),3.30-3.48 (2H, m), 3.48-3.71 (6H, m), 4.51 (2×1/2H, d, J=15 Hz), 4.81(2×1/2H, d, J=15 Hz), 4.70-5.04 (1H, m), 5.15-5.30 (1H, m), 6.99 (1H,s), 7.09 (1H, t, J=8 Hz), 7.16-7.30 (1H, m), 7.39-7.57 (2H, m),7.58-7.85 (3H, m), 7.92 (1H, s), 7.98 (1H, d, J=8 Hz), 8.10 (2H, t, J=8Hz), 8.73 (1×4/5H, s), 8.81 (1×1/5H, s)

(26) MASS: 685 (M+1); NMR (CDCl₃, δ): 0.91 (3H, t, J=8 Hz), 1.63-1.82(2H, m), 2.28 (3H, s), 2.32-2.53 (4H, m), 2.58-2.70 (1H, m), 2.58(3×2/3H, s), 2.73 (3×1/3H, s), 2.93-3.13 (2H, m), 3.33 (1H, dd, J=15, 2Hz), 3.41-3.60 (2H, m), 3.61-3.71 (2H, m), 3.72-3.90 (2H, m), 3.88(2×1/6H, d, J=16 Hz), 3.99 (2×1/3H, d, J=15 Hz), 4.10 (2×1/6H, d, J=16Hz), 4.31 (2×1/3H, d, J=15 Hz), 4.98-5.12 (2H, m), 6.88 (1×1/3H, dd,J=10, 2 Hz), 7.18 (1×2/3H, dd, J=10, 2 Hz), 7.06 (1H, dd, J=10, 2 Hz),7.10-7.30 (6H, m), 7.37-7.49 (2H, m), 7.70 (1×2/3H, d, J=8 Hz), 7.78(1×1/3H, d, J=8 Hz), 7.80-7.90 (3H, m), 8.11 (1×1/3H, d, J=8 Hz), 8.13(1×2/3H, d, J=8 Hz)

(27) MASS: 628 (M+1); NMR (CDCl₃, δ): 2.59 (3×3/4H, s), 2.65 (1H, dd,J=16, 8 Hz), 2.72 (3×1/4H, s), 2.96-3.13 (2H, m), 3.30 (1H, dd, J=15, 2Hz), 3.40-3.58 (2H, m), 3.60-3.80 (6H, m), 3.88 (3H, s), 4.20 (2×1/8H,d, J=16 Hz), 4.21 (2×3/8H, d, J=15 Hz), 4.29 (2×1/8H, d, J=16 Hz), 4.51(2×3/8H, d, J=15 Hz), 5.01-5.22 (2H, m), 6.64 (1×1/4H, d, J=8 Hz), 6.68(1×3/4H, d, J=8 Hz), 7.07-7.37 (7H, m), 7.42 (1H, t, J=8 Hz), 7.50 (1H,s), 7.57 (1H, d, J=8 Hz), 7.68 (1H, d, J=8 Hz), 7.70 (1H, d, J=8 Hz),7.84 (1×1/4H, d, J=2 Hz), 7.93 (1×3/4H, d, J=2 Hz), 8.21 (1H, d, J=8 Hz)

(28) MASS: 627 (M+1); NMR (CDCl₃, δ): 2.53 (3×3/4H, s), 2.61-2.78 (1H,m), 2.73 (3×1/4H, s), 2.90-3.10 (2H, m), 3.18 (1H, d, J=16 Hz),3.28-3.43 (2H, m), 3.44-3.68 (6H, m), 3.87 (3H, s), 3.94 (2×1/8H, d,J=16 Hz), 4.13 (2×3/8H, d, J=15 Hz), 4.24 (2×1/8H, d, J=16 Hz), 4.52(2×3/8H, d, J=15 Hz), 5.02-5.18 (1H, m), 5.19-5.30 (1H, m), 6.60 (1H, d,J=8 Hz), 6.93-7.48 (9H, m), 7.43 (1H, d, J=8 Hz), 7.63 (1H, d, J=8 Hz),7.81 (1×1/4H, s), 7.91 (1×3/4H, s), 8.01-8.22 (2H, m)

(29) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 2.51-2.67 (1H, m), 2.63(3H×2/3, s), 2.82 (3H×1/3, s), 2.97-3.07 (2H, m), 3.23-3.38 (1H, m),3.40-3.59 (2H, m), 3.60-3.80 (6H, m), 4.15 (1H×1/3, d, J=16.5 Hz), 4.31(1H×2/3, d, J=16.5 Hz), 4.40 (1H×1/3, d, J=16.5 Hz), 4.63 (1H×2/3, d,J=16.5 Hz), 5.01-5.16 (2H, m), 6.84 (1H, d, J=2.5 Hz), 6.93-7.21 (7H,m), 7.23-7.33 (3H, m), 7.54 (1H, d, J=7.5 Hz), 7.63-7.83 (3H, m),8.05-8.15 (2H, m)

(30) MASS (m/z): 623 (M+H)⁺ ; NMR (CDCl₃, δ): 2.54-2.70 (1H, m), 2.63(3H×2/3, s), 2.82 (3H×1/3, s), 2.99-3.12 (2H, m), 3.25 (1H×1/3, dd,J=16.0, 3.0 Hz), 3.29 (1H×2/3, dd, J=16.0, 3.0 Hz), 3.41-3.57 (2H, m),3.61-3.77 (6H, m), 4.17 (1H×1/3, d, J=15.0 Hz), 4.31 (1H×2/3, d, J=15.0Hz), 4.39 (1H×1/3, d, J=15.0 Hz), 4.64 (1H×2/3, d, J=15.0 Hz), 4.99-5.18(2H, m), 6.77 (1H, d, J=2.5 Hz), 6.97-7.30 (11H, m), 7.36 (1H, d, J=7.5Hz), 7.44 (2H, t, J=7.5 Hz), 7.60-7.73 (1H, m), 7.75 (2H, t, J=7.5 Hz),8.01 (1H, d, J=7.5 Hz)

(31) MASS (m/z): 597 (M+H)⁺ ; NMR (CDCl₃, δ): 2.42-2.60 (1H, m), 2.63(3H×2/3, s), 2.82 (3H×1/3, s), 2.98-3.77 (13H, m), 4.06-4.69 (3H, m),4.83-5.15 (2H, m), 6.75-7.02 (2H, m), 7.06-7.33 (11H, m), 7.41-7.74 (2H,m), 8.07 (1H×1/3, d, J=8.5 Hz), 8.32 (1H×2/3, d, J=8.5 Hz), 9.23 (1H, brs)

EXAMPLE 42

The following object compounds were obtained according to a similarmanner to that of Example 1.

(1) MASS: 641 (M+1); NMR (CDCl₃, δ): 0.83 (3×1/4H, t, J=8 Hz), 0.87(3×3/4H, t, J=8 Hz), 1.17-1.43 (4H, m), 1.58-1.84 (2H, m), 2.69 (1H, dd,J=16, 7 Hz), 2.91 (3×1/4H, s), 3.02 (3×3/4H, s), 3.30 (1H, dd, J=16, 2Hz), 3.38-3.58 (2H, m), 3.58-3.78 (6H, m), 4.51 (2×3/8H, d, J=15 Hz),4.62 (2×1/8H, d, J=16 Hz), 4.70 (2×3/8H, d, J=15 Hz), 4.78 (2×1/8H, d,J=16 Hz), 4.82-5.00 (1H, m), 5.08-5.20 (1H, m), 7.21-7.33 (1H, m),7.34-7.48 (2H, m), 7.49 (1H, s), 7.55 (1H, d, J=8 Hz), 7.60-7.83 (4H,m), 8.18-8.38 (2H, m), 8.58 (1×3/4H, s), 8.61 (1×1/4H, s), 8.68 (1H, brs), 9.21 (1H, br s)

(2) MAS: 640 (M+1); NMR (CDCl₃, δ): 0.78 (3×1/4H, t, J=8 Hz), 0.80(3×3/4H, t, J=8 Hz), 1.08-1.40 (4H, m), 1.51-1.81 (2H, m), 2.69 (1H, dd,J=16, 4 Hz), 2.89 (3×1/4H, s), 2.93 (3×3/4H, s), 3.30 (1H, dd, J=16, 2Hz), 3.31-3.50 (2H, m), 3.50-3.72 (6H, m), 4.40 (2×3/8H, d, J=15 Hz),4.61 (2×1/8H, d, J=16 Hz), 4.66 (2×3/8H, d, J=15 Hz), 4.69 (2×1/8H, d,J=16 Hz), 4.81-5.01 (1H, m), 5.18-5.30 (1H, m), 6.99 (1H, s), 7.10 (1H,t, J=8 Hz), 7.22 (1H, t, J=8 Hz), 7.30-7.49 (2H, m), 7.56-7.80 (3H, m),7.96 (1H, d, J=8 Hz), 8.11 (1H, d, J=8 Hz), 8.28 (1×3/4H, s), 8.30(1×1/4H, s), 8.51 (1×3/4H, s), 8.59 (1×1/4H, s), 8.63 (1H, s), 9.19 (1H,s)

(3) MASS: 605 (M+1); NMR (CDCl₃, δ): 0.79 (3×1/4H, t, J=8 Hz), 0.80(3×3/4H, t, J=8 Hz), 1.03-1.40 (4H, m), 1.47-1.78 (2H, m), 2.90 (3×1/4H,s), 3.00 (3×3/4H, s), 3.31 (1×1/4H, d, J=6 Hz), 3.39 (1×3/4H, d, J=6Hz), 3.43 (1×1/4H, d, J=4 Hz), 3.50 (1×3/4H, d, J=4 Hz), 4.51 (2×3/8H,d, J=15 Hz), 4.63 (2×1/8H, d, J=16 Hz), 4.68 (2×1/8H, d, J=16 Hz), 4.72(2×3/8H, d, J=15 Hz), 4.81-5.00 (1H, m), 5.03-5.17 (1H, m), 7.19 (1H, t,J=8 Hz), 7.22-7.33 (2H, m), 7.33-7.43 (2H, m), 7.48 (1H, s), 7.51(1×3/4H, s), 7.55 (1×1/4H, s), 7.58-7.81 (4H, m), 8.11 (1H, d, J=8 Hz),8.28 (1×3/4H, d, J=8 Hz), 8.31 (1×1/4H, d, J=8 Hz), 8.50-8.70 (3H, m),8.78 (1×1/4H, d, J=8 Hz), 8.80 (1×3/4H, d, J=8 Hz), 9.18 (1×3/4H, s),9.21 (1×1/4H, s)

(4) MASS: 604 (M+1); NMR (CDCl₃, δ): 0.70 (3×1/5H, t, J=8 Hz), 0.72(3×4/5H, t, J=8 Hz), 0.97-1.30 (4H, m), 1.38-1.53 (1H, m), 1.54-1.70(1H, m), 2.90 (3×1/5H, s), 2.97 (3×4/5H, s), 3.30-3.50 (2H, m), 4.58(2×4/5H, s), 4.61 (2×1/5H, s), 4.89 (1×4/5H, q, J=8 Hz), 4.95 (1×1/5H,q, J=8 Hz), 5.22 (1×4/5H, q, J=8 Hz), 5.31 (1×1/5H, q, J=8 Hz),7.00-7.74 (11H, m), 8.09 (1×4/5H, d, J=8 Hz), 8.30 (1×1/5H, d, J=8 Hz),8.25 (1×4/5H, d, J=8 Hz), 8.36 (1×1/5H, d, J=8 Hz), 8.47-8.60 (2H, m),8.62 (1H, ,d, J=2 Hz), 8.71 (1H, d, J=2 Hz), 9.13 (1×4/5H, s), 9.19(1×1/5H, s)

(5) MASS: 588 (M+1); NMR (CDCl₃, δ): 0.78 (3×1/5H, t, J=8 Hz), 0.81(3×4/5H, t, J=8 Hz), 1.20-1.43 (4H, m), 1.57-1.90 (2H, m), 2.08 (3H, s),2.13-2.27 (2H, m), 2.64 (2H, t, J=8 Hz), 3.00 (3×1/5H, s), 3.04 (3×4/5H,s), 4.60-4.82 (2H, m), 4.92-5.07 (2H, m), 7.20-7.84 (10H, m), 8.32 (1H,d, J=8 Hz), 8.62 (1H, s), 8.63-8.78 (1H, m), 9.24 (1H, s)

(6) MASS: 587 (M+1); NMR (CDCl₃, δ): 0.61 (3×1/5H, t, J=8 Hz), 0.65(3×4/5H, t, J=8 Hz), 1.03-1.40 (4H, m), 1.56-1.90 (2H, m), 2.03 (3H, s),2.14-2.40 (2H, m), 2.63 (2H, t, J=8 Hz), 3.14 (3×1/5H, s), 3.17 (3×4/5H,s), 4.64-4.96 (2H, m), 5.18 (1H, q, J=8 Hz), 5.52 (1H, q, J=8 Hz),7.00-7.50 (7H, m), 7.64 (1H, d, J=8 Hz), 7.68-7.85 (2H, m), 8.34 (1H, d,J=8 Hz), 8.64 (1H, s), 8.82 (1×4/5H, d, J=8 Hz), 8.97 (1×1/5H, d, J=8Hz), 9.22 (1H, s)

(7) MASS (m/z): 578 (M⁺ +1); NMR (CDCl₃, δ): 0.81 (3H, t, J=7 Hz), 1.26(4H, m), 1.63 (2H, m), 2.50 (3H, s), 2.57-2.65 (1H, m), 2.81 (3H×1/4,s), 2.93 (3H×3/4, s), 3.22-3.27 (1H, m), 3.42 (2H, m), 3.60 (6H, m),4.32 (1H×3/4, d, J=15 Hz), 4.50 (1H×1/4, d, J=16 Hz), 4.61 (1H×1/4, d,J=16 Hz), 4.63 (1H×3/4, d, J=15 Hz), 4.83 (1H, m), 5.06 (1H, m),7.05-7.26 (2H, m), 7.35-7.51 (4H, m), 7.61-7.69 (2H, m), 8.20 (1H, m),8.29-8.34 (1H, m)

(8) MASS (m/z): 577 (M⁺ +1); NMR (CDCl₃, δ): 0.77 (3H, t, J=7 Hz), 1.27(4H, m), 1.64 (2H, m), 2.51 (3H, s), 2.67 (1H, m), 2.82 (3H×1/4, s),2.90 (3H×3/4, s), 3.22-3.28 (1H, m), 3.37 (2H, m), 3.58 (6H, m), 4.27(1H×3/4, d, J=15 Hz), 4.53 (2H×1/4, s), 4.62 (1H×3/4, d, J=15 Hz), 4.86(1H, m), 5.18 (1H, m), 6.98 (1H, m), 7.04-7.13 (2H, m), 7.25 (1H, m),7.40-7.45 (2H, m), 7.62 (1H, m), 7.90 (1H, m), 8.10 (1H, m), 8.30-8.37(1H, m)

(9) MASS (m/z): 542 (M⁺ +1); NMR (CDCl₃, δ): 0.75 (3H, t, J=7 Hz), 1.11(4H, m); 1.48 (1H, m), 1.60 (1H, m), 2.45 (3H, s), 2.80 (3H×1/3, s),2.92 (3H×2/3, s), 3.28-3.46 (2H, m), 4.31 (1H×2/3, d, J=15 Hz), 4.54(2H×1/3, s), 4.62 (1H×2/3, d, J=15 Hz), 4.83 (1H, m), 5.07 (1H, m),7.03-7.27 (4H, m), 7.37-7.62 (6H, m), 8.06 (1H, m), 8.29 (1H, m), 8.53(1H, m), 8.73 (1H, m)

(10) MASS (m/z): 541 (M⁺ +1); NMR (CDCl₃, δ): 0.74 (3H, t, J=7 Hz), 1.09(4H, m), 1.42 (1H, m), 1.60 (1H, m), 2.53 (3H, s), 2.92 (3H, s), 3.38(2H, m), 4.49 (2H, s), 4.87 (1H, m), 5.19 (1H, m), 7.08-7.37 (7H, m),7.39-7.53 (3H, m), 7.65 (1H, m), 7.97 (1H, m), 8.32 (1H, m), 8.52 (1H,m), 8.65 (1H, m)

(11) MASS (m/z): 525 (M⁺ +1); NMR (CDCl₃, δ): 0.80 (3H, t, J=7 Hz), 1.29(4H, m), 1.62 (1H, m), 1.72 (1H, m), 2.10 (3H, s), 2.14-2.20 (2H, m),2.52 (3H, s), 2.60 (2H, m), 2.91 (3H×1/4, s), 3.01 (3H×3/4, s), 4.47(1H×3/4, d, J=15 Hz), 4.56 (1H×1/4, d, J=16 Hz), 4.66 (1H×3/4, d, J=15Hz), 4.66 (1H×1/4, d, J=16 Hz), 4.93 (2H, m), 7.11 (1H, m), 7.21-7.47(7H, m), 7.63-7.65 (1H, m), 8.35-8.40 (1H, m)

(12) MASS (m/z): 524 (M⁺ +1); NMR (CDCl₃, δ): 0.66 (3H, t, J=7 Hz), 1.22(4H, m), 1.63 (1H, m), 1.74 (1H, m), 2.05 (3H, s), 2.17 (2H, m), 2.55(3H, s), 2.62 (2H, m), 3.10 (3H, s), 4.64 (1H, d, J=15 Hz), 4.83 (1H, d,J=15 Hz), 5.13 (1H, m), 5.50 (1H, m), 7.02-7.33 (6H, m), 7.45-7.64 (2H,m), 8.43 (1H, m), 8.79 (1H, m) (13) MASS (m/z): 481 (M³⁰ +1); NMR(CDCl₃, δ): 0.83 (3H, t, J=7 Hz), 1.33 (4H, m), 1.72 (2H, m), 2.49(3H×5/6, s), 2.55 (3H×1/6, s), 2.89 (3H×1/4, s), 3.03 (3H×3/4, s), 3.77(1H, m), 4.09 (1H, m), 4.54 (2H, m), 4.95 (3H, m), 7.04-7.49 (5H, m),7.61-7.77 (3H, m), 8.30-8.42 (1H, m)

(14) MASS (m/z): 480 (M⁺ +1); NMR (CDCl₃, δ): 0.81 (3H, t, J=7 Hz), 1.31(4H, m), 1.73 (1H, m), 1.93 (1H, m), 2.38 (3H, s), 3.03 (3H×1/6, s),3.15 (3H×5/6, s), 3.97 (2H, m), 4.38 (1H, d, J=15 Hz), 4.87 (1H, d, J=15Hz), 5.08 (1H, m), 5.62 (1H, m), 6.72 (1H, m), 6.95 (1H, m), 7.07-7.36(6H, m), 7.61 (1H, m), 8.27 (1H×5/6, m), 8.38 (1H×1/6, m), 9.09 (1H, m)

(15) MASS (m/z): 641 (M⁺ +1); NMR (CDCl₃, δ): 2.30 (3H, s),2.33-2.58(4H, m), 2.60 (3×3/4H, s), 2.68 (1H, dd, J=17 and 8 Hz), 2.79(3×1/4H, s), 2.98-3.12 (2H, m), 3.23-3.40 (1H, m), 3.40-3.60 (2H, m),3.62-3.75 (2H, m), 3.82 (3H, s), 3.90 (2×1/8H, d, J=16 Hz), 4.38(2×1/8H, d, J=16 Hz), 4.41 (2×3/8H, d, J=15 Hz), 4.49 (2×3/8H, d, J=15Hz), 5.01-5.20 (2H, m), 7.07 (1H, s), 7.11-7.38 (6H, m), 7.43 (1H, t,J=8 Hz), 7.50 (1H, s), 7.58 (1H, d, J=8 Hz), 7.69 (1H, d, J=8 Hz), 7.80(1×3/4H, d, J=8 Hz), 7.84 (1×1/4H, d, J=8 Hz), 7.90 (1×1/4H, s), 8.00(1×3/4H, s), 8.13-8.30 (2H, m)

(16) MASS (m/z): 640 (M⁺ +1); NMR (CDCl₃, δ): 2.21 (3H, s), 2.27-2.40(4H, m), 2.56 (3×3/4H, s), 2.69 (1H, dd, J=17 and 6 Hz), 2.73 (3×1/4H,s), 2.92-3.10 (2H, m), 3.11-3.27 (1H, m), 3.30-3.48 (2H, m), 3.50-3.70(2H, m), 3.72 (3×3/4H, s), 3.78 (3×1/4H, s), 3.93 (2×1/8H, d, J=16 Hz),4.30 (2×1/8H, d, J=16 Hz), 4.31 (2×3/8H, d, J=15 Hz), 4.47 (2×3/8H, d,J=15 Hz), 5.08 (1H, q, J=8 Hz), 5.17-5.26 (1H, m), 6.90-7.20 (8H, m),7.21 (1Hi d, J=8 Hz), 7.42 (1H, d, J=8 Hz), 7.62 (1H, d, J=8 Hz), 7.87(1×1/4H, s), 7.97 (1×3/4H, s), 8.02-8.17 (2H, m), 8.20 (1H, s)

(17) NMR (CDCl₃, δ): 2.29 (3H, s), 2.32-2.55 (4H, m), 2.62-2.74 (1H, m),2.68 (3×2/3H, s), 2.70 (3×1/3H, s), 2.98-3.18 (2H, m), 3.27-3.42 (1H,m), 3.43-3.60 (2H, m), 3.61-3.72 (2H, m), 3.82 (3H, s), 3.56 (2×1/6H, d,J=16 Hz), 4.33 (2×1/3H, d, J=15 Hz), 4.38 (2×1/6H, d, J=16 Hz), 4.60(2×1/3H, d, J=15 Hz), 5.04-5.14 (1H, m), 5.10 (1×2/3H, q, J=8 Hz), 5.39(1×1/3H, q, J=8 Hz), 6.72 (1H, d, J=7 Hz), 7.10-7.32 (6H, m), 7.41 (1H,t, J=8 Hz), 7.49 (1H, s), 7.53-7.82 (3H, m), 8.03 (1×1/3H, s), 8.20(1×2/3H, s), 8.18-8.30 (1H, m), 8.41 (1H, dd, J=7, 2 Hz)

(18) NMR (CDCl₃, δ): 2.22 (3H, s), 2.29-2.48 (4H, m), 2.61-2.80 (1H, m),2.69 (3×2/3H, s), 2.71 (3×1/3H, s), 2.90-3.12 (2H, m), 3.13-3.33 (1H,m), 3.35-3.50 (2H, m), 3.51-3.71 (2H, m), 3.73 (3×1/3H, s), 3.76(3×2/3H, s), 3.70 (2×1/6H, d, J=16 Hz), 4.37 (2×1/6H, d, J=16 Hz), 4.42(2×1/3H, d, J=15 Hz), 4.52 (2×1/3H, d, J=15 Hz), 5.08-5.25 (1H, m), 5.18(1×2/3H, q, J=8 Hz), 5.41 (1×1/3H, q, J=8 Hz), 6.65-6.78 (1H, m), 6.99(1H, s), 7.00-7.20 (5H, m), 7.21 (1H, d, J=8 Hz), 7.27 (1H, s), 7.42(1H, d, J=8 Hz), 7.62 (1H, d, J=8 Hz), 7.91-8.09 (2H, m), 8.10 (1×1/3H,s), 8.20 (1×2/3H, s), 8.37-8.50 (1H, m)

(19) MASS: 705 (M+1); NMR (CDCl₃, δ): 2.28 (3H, s), 2.32-2.52 (4H, m),2.58-2.72 (1H, m), 2.60 (3×3/4H, s), 2.77 (3×1/4H, s), 2.96-3.12 (2H,m), 3.31 (1H, dd, J=16, 2 Hz), 3.40-3.60 (2H, m), 3.61-3.80 (2H, m),4.02 (2×1/8H, d, J=16 Hz), 4.30 (2×3/8H, d, J=15 Hz), 4.33 (2×3/8H, d,J=15 Hz), 4.54 (2×1/8H, d, J=16 Hz), 4.97-5.11 (2H, m), 7.10-7.23 (5H,m), 7.35-7.49 (2H, m), 7.51 (1×1/4H, s), 7.68 (1×3/4H, s), 7.78-7.90(4H, m), 8.11 (1×3/4H, d, J=8 Hz), 8.18 (1×1/4H, d, J=8 Hz), 8.30 (1H,s), 8.59 (1H, s)

EXAMPLE 43

A mixture of Starting Compound (209 mg) and O-methyl benzob!furan-2-carbothioate (104 mg) in methanol (2.5 ml) was stirred at roomtemperature for 3 hours. The solvent was evaporated, and the residue waspurified by column chromatography (silica gel, chloroform/methanol=70/1)to give Object Compound (121 mg) as yellow powder.

MASS (m/z): 578 (M+H)⁺ ; NMR (CDCl₃, δ): 2.63 (4/5×3H, s), 2.77 (1/5×3H,s), 2.85-3.08 (2H, m), 3.25-3.42 (1H, m), 3.50-3.66 (1H, m), 4.23(1/5×2H, ABq, Δ=0.20, J=17 Hz), 4.45 (4/5×2H, ABq, Δ=0.19, J=15 Hz),5.05-5.21 (1H, m), 5.41-5.58 (1H, m), 7.05-7.80 (16H, m), 8.23-8.82 (4H,m)

EXAMPLE 44

The following compounds were obtained according to a similar manner tothat of Example 1.

(1) MASS (m/z): 559 (M+H)⁺ ; NMR (CDCl₃, δ): 1.60-2.05 (2H, m), 1.88(1/4×3H, s), 1.94 (3/4×3H, s), 2.12-2.40 (2H, m), 2.54 (1/4×3H, s), 2.58(3/4×3H, s), 2.87 (1/4×3H, s), 2.99 (3/4×3H, s), 3.25-3.52 (2H, m), 4.52(3/4×2H, ABq, Δ=0.26, J=15 Hz), 4.60 (1/4×2H, ABq, Δ=0.08, J=17 Hz),4.96-5.24 (2H, m), 7.00-7.80 (11H, m), 8.27-8.80 (3H, m), 10.50 (1H, brs)

(2) MASS (m/z): 560 (M+H)⁺ ; NMR (CDCl₃, δ): 1.70-2.05 (2H, m), 1.93(1/4×3H, s), 1.98 (3/4×3H, s), 2.20-2.40 (2H, m), 2.51 (3/4×3H, s), 2.55(1/4×3H, s), 2.83 (1/4×3H, s), 2.98 (3/4×3H, s), 3.23-3.56 (2H, m), 4.51(3/4×2H, ABq, Δ=0.27, J=15 Hz), 4.60 (1/4×2H, ABq, Δ=0.13, J=17 Hz),4.95-5.18 (2H, m), 7.02-7.72 (10H, m), 8.02-8.83 (4H, m)

(3) MASS (m/z): 498 (M+H)⁺ ; NMR (CDCl₃, δ): 1.92-2.32 (2H, m), 1.97(1/5×3H, s), 2.06 (4/5×3H, s), 2.39 (3H, m), 2.42-2.70 (2H, s), 3.08(1/5×3H, s), 3.25 (4/5×3H, s), 3.85-4.08 (2H, m), 4.30 (4/5×1H, d, J=15Hz), 4.52 (1/5×1H, d, J=17 Hz), 4.91 (1/5×1H, d, J=17 Hz), 4.97 (4/5×1H,d, J=15 Hz), 5.23-5.67 (2H, m), 6.62-7.68 (8H, m), 8.25 (4/5×1H, s),8.43 (1/5×1H, s), 9.02 (1/5×1H, d, J=9 Hz), 9.16 (4/5×1H, d, J=9 Hz),10.50 (1H, br s)

(4) MASS (m/z): 4 99 (M+H)⁺ ; NMR (CDCl₃, δ): 1.80-2.15 (2H, m), 1.98(1/4×3H, s), 2.06 (3/4×3H, s), 2.45-2.67 (2H, m), 2.50 (3H, s), 2.92(1/4×3H, s), 3.08 (3/4×3H, s), 3.68-3.88 (1H, m), 4.02-4.22 (1H, m),4.48 (1/4×1H, d, J=17 Hz), 4.56 (3/4×2H, ABq, Δ=0.06, J=15 Hz), 4.68(1H, br s), 4.80-5.28 (2H, m), 4.83 (1/4×1H, d, J=17 Hz), 7.00-7.78 (9H,m), 8.32 (3/4×1H, s), 8.43 (1/4×1H, s)

(5) MASS (m/z): 595 (M+H)⁺ ; NMR (CDCl₃, δ): 1.80-2.07 (2H, m), 1.99(3H×1/5, s), 2.04 (3H×4/5, s), 2.47-2.59 (2H, m), 2.56 (3H, s), 2.63(1H, dd, J=16.0, 6.0 Hz), 2.85 (3H×1/5, s), 2.99 (3H×4/5, s), 3.35 (1H,dd, J=16.0, 3.0 Hz), 3.41-3.52 (2H, m), 3.58-3.77 (6H, m), 4.41 (1H×4/5,d, J=15 Hz), 4.51 (1H×1/5, d, J=16.0 Hz), 4.56 (1H×4/5, d, J=15.0 Hz),4.70 (1H×1/5, d, J=16.0 Hz), 5.04-5.22 (2H, m), 7.00 (1H, d, J=1.0 Hz),7.09-7.21 (2H, m), 7.30 (1H, t, J=7.5 Hz), 7.40-7.52 (2H, m), 7.69 (2H,t, J=7.5 Hz), 8.04 (1H, d, J=7.5 Hz), 8.31 (1H×4/5, d, J=1.0 Hz), 8.39(1H×1/5, d, J=1.0 Hz), 9.34 (1H×1/5, br s), 9.70 (1H×4/5, br s)

(6) MASS (m/z): 596 (M+H)⁺ ; NMR (CDCl₃, δ): 1.82-2.07 (2H, m), 2.02(3H×1/4, s), 2.10 (3H×3/4, s), 2.50-2.70 (3H, m), 2.53 (3H, s), 2.87(3H×1/4, s), 3.04 (3H×3/4, s), 3.29-3.57 (3H, m), 3.60-3.78 (6H, m),4.40 (1H×3/4, d, J=15.0 Hz), 4.53 (1H×1/4, d, J=16.0 Hz), 4.67 (1H×3/4,d, J=15.0 Hz), 4.75 (1H×1/4, d, J=16.0 Hz), 5.06-5.26 (2H, m), 7.12(1H×3/4, d, J=7.5 Hz), 7.21 (1H×1/4, d, J=7.5 Hz), 7.31 (1H, t, J=7.5Hz), 7.44 (2H, t, J=7.5 Hz), 7.51 (1H, s), 7.58 (1H, d, J=7.5 Hz),7.66-7.74 (2H, m), 8.21 (1H, d, J=7.5 Hz), 8.35 (1H×3/4, d, J=1.0 Hz),8.40 (1H×1/4, d, J=1.0 Hz)

(7) MASS (m/z): 542 (M+H)⁺ ; NMR (CDCl₃, δ): 1.72-2.31 (4H, m), 1.88(3H×1/4, s), 1.91 (3H×3/4, s), 2.09 (3H, s), 2.39-2.54 (2H, m),2.57-2.69 (2H, m), 2.58 (3H, s), 3.08 (3H×1/4, s), 3.15 (3H×3/4, s),4.62 (1H×1/4, d, J=16.0 Hz), 4.69 (1H×3/4, d, J=15.0 Hz), 4.73 (1H×3/4,d, J=15.0 Hz), 4.88 (1H×1/4, d, J=16.0 Hz), 5.23-5.42 (2H, m), 6.99 (1H,s), 7.09-7.25 (4H, m), 7.40 (1H, d, J=7.5 Hz), 7.52 (1H, m), 7.67 (1H,d, J=7.5 Hz), 8.44 (1H, s), 8.47 (1H×3/4, d, J=7.5 Hz), 8.61 (1H×1/4, d,J=7.5 Hz), 10.10 (1H, br s)

(8) MASS (m/z): 543 (M+H)⁺ ; NMR (CDCl₃, δ): 1.83-2.27 (4H, m), 1.99(3H×1/4, s), 2.04 (3H×3/4, s), 2.17 (3H, s), 2.43-2.76 (4H, m), 2.55(3H, s), 2.91 (3H×1/4, s), 3.07 (3H×3/4, s), 4.49 (1H×3/4, d, J=15.0Hz), 4.60 (1H×1/4, d, J=16.0 Hz), 4.65 (1H×3/4, d, J=15.0 Hz), 4.79(1H×1/4, d, J=16.0 Hz), 4.83-4.96 (1H, m), 5.06-5.27 (1H, m), 7.05-7.23(2H, m), 7.24-7.36 (1H, m), 7.37-7.57 (5H, m), 7.68 (1H, d, J=7.5 Hz),8.37 (1H×3/4, s), 8.40 (1H×1/4, s)

We claim:
 1. A compound of the formula: ##STR2152## wherein: W is benzofuryl or benzothienyl;A¹ is >C=V, wherein V is O or S; T is pyridyl; A² is lower alkylene; R⁸ is hydrogen or lower alkyl; R³ is aryl, which is optionally substituted; A³ is a direct bond or lower alkylene; R⁹ is hydrogen or lower alkyl; R⁴ has the formula ##STR2153## wherein R⁵ is hydrogen or lower alkyl; and R⁶ is pyridyl lower alkyl; or a pharmaceutically acceptable salt thereof.
 2. The compound of claim 1, wherein W is benzofuryl.
 3. The compound of claim 1, wherein W is benzothienyl.
 4. The compound of claim 1, wherein A² is C₁ - or C₂ -alkylene.
 5. The compound of claim 1, wherein R⁸ is hydrogen.
 6. The compound of claim 1, wherein R⁹ is hydrogen.
 7. The compound of claim 1, wherein R⁵ of group R⁴ is hydrogen.
 8. The compound of claim 1, wherein R³ is phenyl or naphthyl each of which are optionally substituted by lower alkyl, lower alkoxy, lower alkenyl, lower alkynyl, mono-, di-, tri-halo (lower) alkyl, cyclo(lower)alkyl, cyclo(lower) alkenyl, halogen, carboxy, protected carboxy, hydroxy, protected hydroxy, phenyl, napthyl, ar(lower)alkyl, carboxy(lower) alkyl, protected carboxy(lower) alkyl, nitro, amino, protected amino, di(lower) alkylamino, amino (lower)alkyl, protected amino(lower)alkyl, cyano, sulfo, oxo, sulfamoyl, carbamoyloxy, mercapto, lower alkylthio and methylenedioxy.
 9. The compound of claim 1, which is in the form of a salt, said salt being a salt of an inorganic base.
 10. The compound of claim 1, which is in a form of a salt, said salt being a salt of an organic amine.
 11. The compound of claim 1, which is in a form of a salt, said salt being a salt of an inorganic acid.
 12. The compound of claim 1, which is in a form of a salt, said salt being a salt of a basic or acidic amino acid.
 13. A method of inhibiting production of nitric oxide (NO) in a mammal, which comprises administrating to said mammal an effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof.
 14. The method of claim 13, wherein said mammal is a human. 